SlideShare a Scribd company logo
NUCLEAR RECEPTOS & CHEMICAL TRANSMISSION AND DRUG
ACTION IN THE CNS
Introduction
Structure
Mechanism of
Action
Classification of
Psychotropic Drug
Targets for Drugs
Action
Drug in CNS
NUCLEAR RECEPTORS
“Nuclear receptors are a family of highly conserved transcription in response to small
lipophilic compound.”
Play important role in development, physiology and disease in humans by regulating
gene expression (Protein or amino acid formation)
Estrogen or β-estradiol act upon the nuclear receptor to regulate gene expression for
Female Sex Development
Testosterone or Androgens act upon nuclear receptors to regulate gene expression for
Male Sex Development
STRUCTURE
All nuclear are monomeric proteins
Share broadly similar structural design
It has six domains (A-F):
(A-B) N-regulatory domain
(C) DNA binding domain
(D) Hinge Region
(E) Ligand binding domain
(F) C-terminal domain
STRUCTURE
(A-B) N-regulatory domain: Highly variable in sequence between various nuclear receptors
(C) DNA binding domain: Highly conserved, contain two zinc fingers that bind to specific DNA sequences
(D) Hinge Region: Flexible domain
(E) Ligand binding domain: it is alpha helical sandwich fold, three anti-parallel helices flanked by two alpha helices on
one side and three on the other, binding cavity is within the inferior of the LBD and just below three anti-parallel alpha
helical sandwich
(F) C-terminal domain: Highly variable sequence, Near to it are located the motifs that contain nuclear localization
signals
FUNCTIONS OF THE DOMAINS
N-terminal domain: harbors AF1 site that binds to other cell specific transcription factors in a
ligand-independent way and modifies the binding or activity of the receptor
DNA binding domain: Binds to the specific sequences of DNA called hormone response element
Hinge region: Connects the DNA binding domain to the ligand binding domain
Ligand binding domain: Harbors the AF2 whose action depends upon the bound ligand
C-terminal domain: has ability to the transcription
MECHANISM OF ACTION
Classes
Class I nuclear
receptors
Class II nuclear
receptors
Class III nuclear
receptors
MECHANISM OF ACTION
Class I Nuclear Receptors: Largely steroid receptors
Ligands are mainly steroids
Located in cytoplasm or attached to cytoskeleton or other structures
When ligand binds, form homodimers in the presence of their partners and migrate to nucleus
to trigger signal response
A single ligand can regulate a large number of genes
MECHANISM OF ACTION
Class II Nuclear Receptors: Their ligands are mainly lipids
Located in nucleus
They form heterodimers with retinoid X receptors
Class III Nuclear Receptors: They transduce endocrine signals but function
as heterodimers
CHEMICAL TRANSMISSION AND DRUG ACTION IN THE CNS
INTRODUCTION
• Drugs acting on CNS are of special significance and
of major therapeutic use but also the drugs which are
commonly administered for non-medical reasons like
coffee, tea and nicotine
• CNS is functionally more complex. Behavior of drug
on the individual cell of brain is different from the
whole brain unlike the other organs
Two reasons for
understanding
the action of
drugs on CNS is
difficult:
CHEMICAL SIGNALING IN THE CNS
CNS produce neurotransmitter
which start processes in the body
and control the biological
functions
It is important to study the
physiology of brain and to study
chemical signaling because whole
body is linked with it.
Drug acting upon CNS will also
produce effects on the body.
For Example,
Adrenaline, controls the
eyes and little bit
dryness of mouth
Dopamine, disturbance
in its release leads to
Parkinson’s disease
GABA, is related to
anxiety
CHEMICAL SIGNALING IN THE CNS
CHEMICAL SIGNALING IN THE CNS
Neurotransmitters control various process in the body in a range of different time scales. The time scale may be in
Miliseconds
Minutes
Hours
Days
Months
Year
Brain system works like a candy floss into the grand canyon
Candy floss mean number of threads that are placed on a stick and enter into a grand canyon
TARGETS FOR DRUG ACTION
Targets for
drug action
Receptors Enzymes Ion channels
Carrier
Molecules
Receptors
• A protein that recognizes the body’s natural mediator or the drug
• When ligand will bind, it transmits signal and elicits a biological effect
Ion channels
• Ion channels are proteins in membrane that allow passage of specific ions only when activated
• Upon receiving signals, it will open and allows the ions to pass
Enzymes
• Biological catalysts that speed up chemical reaction without being changed
• Many drugs act by inhibiting the action of enzymes
Carrier molecules
• Membrane bounded proteins that transport specific molecules
• Molecule to be transported binds to specific protein for recognition site on the carrier and then molecule is transferred to other
side of membrane
TARGETS FOR DRUG ACTION
DRUG ACTION IN CNS
Study action of drug on brain is difficult due to complexity of neuronal
interconnections in the brain
Difficult to predict effects of blocking or enhancing release or action of
one or other neurotransmitters greatly depend upon
External inputs
Influence of glial cells
Range of secondary adaptive responses
Blood brain barrier
Drug transport to specific
target in brain
Direct penetration
Small non-polar molecules
diffuse passively across cell
membrane
Penetration via
transporters
Transporters facilitate entry
into brain
DRUG ACTION IN CNS
CLASSIFICATION OF PSYCHOTROPIC DRUGS
Anaesthetic
agents
• Used to produce surgical anesthesia
• For example, halothane, propofol
Anxiolytic
and
Sedatives
• Used to induce sleep and reduce anxiety
• Hypnotics, sedatives, minor tranquilizers
• For example, barbiturates, benzodiazepines
Antipyschoti
cs drugs
• Used to relieve schizophrenic illness
• Neuroleptics, major tranquilizers
• Clozapine, chlorpronazine
Antidepressa
nt drugs
• Used to relieve depressive illness
• Thymoleptics
• Escitalopram
Analgesic drugs
• Used to relieve from pain
• For example, opiates and carbamazepine
Psychomotor
stimulants
• Used to induce wakefulness and euphoria
• Psychostimulants
• For example, amphetamine, cocaine, caffeine
Psychotomimetic
drugs
• Used to cause disturbance of perception
• Hallucinogens, psychodysleptics
• For example, mesacline, phencyclidine
Cognition
enhancers
• Used to improve memory and cognitive performance
• Nootropic drugs
• For example, tacrine, donepezil
CLASSIFICATION OF PSYCHOTROPIC DRUGS
Some drugs defy this classification
For example, lithium, dissociative anesthetic, used in the
treatment of manic depressive psychosis and ketamine
It produces psychotropic effect rather similar to those produced
by phecyclidine
CLASSIFICATION OF PSYCHOTROPIC DRUGS
Nuclear receptors and chemical action in cns

More Related Content

What's hot

Secondary messengers system
Secondary messengers systemSecondary messengers system
Secondary messengers system
FoziyaKhan
 
GABA, glutamate receptors and their modulation
GABA, glutamate receptors and their modulationGABA, glutamate receptors and their modulation
GABA, glutamate receptors and their modulation
DrSahilKumar
 
opioid autocoids
opioid autocoidsopioid autocoids
opioid autocoids
ARIKILLASUSHMA
 
Genetic variations in gpcr
Genetic variations in gpcrGenetic variations in gpcr
Genetic variations in gpcr
Meenakshi Gupta
 
Receptors and receptors classification
Receptors and receptors classificationReceptors and receptors classification
Receptors and receptors classification
caucasus international university
 
Theoretical basis and optimization of immunoassay
Theoretical basis and optimization of immunoassayTheoretical basis and optimization of immunoassay
Theoretical basis and optimization of immunoassay
AkankshDas
 
Immunoassay of digoxin
Immunoassay of digoxinImmunoassay of digoxin
Immunoassay of digoxin
Rashmi116
 
Cell signaling
Cell signalingCell signaling
Cell signaling
Pavana K A
 
Nuclear Receptors
Nuclear ReceptorsNuclear Receptors
Nuclear Receptors
Arslan Tahir
 
Neurotransmitters/General aspect and steps involved in neurotransmission.pptx
Neurotransmitters/General aspect and steps involved in neurotransmission.pptxNeurotransmitters/General aspect and steps involved in neurotransmission.pptx
Neurotransmitters/General aspect and steps involved in neurotransmission.pptx
SIRAJUDDIN MOLLA
 
Non adrenergic and Non cholinergic transmission
Non adrenergic and Non cholinergic transmission Non adrenergic and Non cholinergic transmission
Non adrenergic and Non cholinergic transmission
E Poovarasan
 
QSAR statistical methods for drug discovery(pharmacology m.pharm2nd sem)
QSAR statistical methods for drug discovery(pharmacology m.pharm2nd sem)QSAR statistical methods for drug discovery(pharmacology m.pharm2nd sem)
QSAR statistical methods for drug discovery(pharmacology m.pharm2nd sem)
Satigayatri
 
Glycine receptor
Glycine receptorGlycine receptor
Glycine receptor
Ruchita Bhavsar
 
Anti-Ischemics | Mechanism | Ischemia | Signs & Symptoms
Anti-Ischemics | Mechanism | Ischemia | Signs & SymptomsAnti-Ischemics | Mechanism | Ischemia | Signs & Symptoms
Anti-Ischemics | Mechanism | Ischemia | Signs & Symptoms
Chetan Prakash
 
Drug receptor interaction
Drug receptor interactionDrug receptor interaction
Drug receptor interaction
Fariha Shikoh
 
Cloning of disease gene
Cloning of disease geneCloning of disease gene
Cloning of disease gene
Bharat Kumar
 
Genetic variation in drug transporters
Genetic variation in drug transportersGenetic variation in drug transporters
Genetic variation in drug transporters
Deepak Kumar
 
Role of genomics and proteomics
Role of genomics and proteomicsRole of genomics and proteomics
Role of genomics and proteomics
Pavana K A
 
Economics of drug discovery. final.pptx
Economics of drug discovery. final.pptxEconomics of drug discovery. final.pptx
Economics of drug discovery. final.pptx
ashharnomani
 
Rationale of prodrug design and practical consideration of
Rationale of prodrug design and practical consideration ofRationale of prodrug design and practical consideration of
Rationale of prodrug design and practical consideration of
College of Pharmacy,Sri Ramakrishna Institute of Paramedical Sciences,Coimbatore
 

What's hot (20)

Secondary messengers system
Secondary messengers systemSecondary messengers system
Secondary messengers system
 
GABA, glutamate receptors and their modulation
GABA, glutamate receptors and their modulationGABA, glutamate receptors and their modulation
GABA, glutamate receptors and their modulation
 
opioid autocoids
opioid autocoidsopioid autocoids
opioid autocoids
 
Genetic variations in gpcr
Genetic variations in gpcrGenetic variations in gpcr
Genetic variations in gpcr
 
Receptors and receptors classification
Receptors and receptors classificationReceptors and receptors classification
Receptors and receptors classification
 
Theoretical basis and optimization of immunoassay
Theoretical basis and optimization of immunoassayTheoretical basis and optimization of immunoassay
Theoretical basis and optimization of immunoassay
 
Immunoassay of digoxin
Immunoassay of digoxinImmunoassay of digoxin
Immunoassay of digoxin
 
Cell signaling
Cell signalingCell signaling
Cell signaling
 
Nuclear Receptors
Nuclear ReceptorsNuclear Receptors
Nuclear Receptors
 
Neurotransmitters/General aspect and steps involved in neurotransmission.pptx
Neurotransmitters/General aspect and steps involved in neurotransmission.pptxNeurotransmitters/General aspect and steps involved in neurotransmission.pptx
Neurotransmitters/General aspect and steps involved in neurotransmission.pptx
 
Non adrenergic and Non cholinergic transmission
Non adrenergic and Non cholinergic transmission Non adrenergic and Non cholinergic transmission
Non adrenergic and Non cholinergic transmission
 
QSAR statistical methods for drug discovery(pharmacology m.pharm2nd sem)
QSAR statistical methods for drug discovery(pharmacology m.pharm2nd sem)QSAR statistical methods for drug discovery(pharmacology m.pharm2nd sem)
QSAR statistical methods for drug discovery(pharmacology m.pharm2nd sem)
 
Glycine receptor
Glycine receptorGlycine receptor
Glycine receptor
 
Anti-Ischemics | Mechanism | Ischemia | Signs & Symptoms
Anti-Ischemics | Mechanism | Ischemia | Signs & SymptomsAnti-Ischemics | Mechanism | Ischemia | Signs & Symptoms
Anti-Ischemics | Mechanism | Ischemia | Signs & Symptoms
 
Drug receptor interaction
Drug receptor interactionDrug receptor interaction
Drug receptor interaction
 
Cloning of disease gene
Cloning of disease geneCloning of disease gene
Cloning of disease gene
 
Genetic variation in drug transporters
Genetic variation in drug transportersGenetic variation in drug transporters
Genetic variation in drug transporters
 
Role of genomics and proteomics
Role of genomics and proteomicsRole of genomics and proteomics
Role of genomics and proteomics
 
Economics of drug discovery. final.pptx
Economics of drug discovery. final.pptxEconomics of drug discovery. final.pptx
Economics of drug discovery. final.pptx
 
Rationale of prodrug design and practical consideration of
Rationale of prodrug design and practical consideration ofRationale of prodrug design and practical consideration of
Rationale of prodrug design and practical consideration of
 

Viewers also liked

Nuclear Receptors
Nuclear ReceptorsNuclear Receptors
Image receptors & accessories
Image receptors & accessoriesImage receptors & accessories
Image receptors & accessories
Indian dental academy
 
Transcription Regulation in Eukaryotes
Transcription Regulation in EukaryotesTranscription Regulation in Eukaryotes
Transcription Regulation in Eukaryotes
IshaqueAbdulla
 
Regulation of Gene Expression ppt
Regulation of Gene Expression pptRegulation of Gene Expression ppt
Regulation of Gene Expression ppt
Khaled Elmasry
 
Receptors
ReceptorsReceptors
Receptors
Raju Sanghvi
 
Receptor Pharmacology
Receptor PharmacologyReceptor Pharmacology
Receptor Pharmacology
Tulasi Raman
 
Drug receptors in pharmacology
Drug receptors in pharmacologyDrug receptors in pharmacology
Drug receptors in pharmacology
Bindu Pulugurtha
 

Viewers also liked (7)

Nuclear Receptors
Nuclear ReceptorsNuclear Receptors
Nuclear Receptors
 
Image receptors & accessories
Image receptors & accessoriesImage receptors & accessories
Image receptors & accessories
 
Transcription Regulation in Eukaryotes
Transcription Regulation in EukaryotesTranscription Regulation in Eukaryotes
Transcription Regulation in Eukaryotes
 
Regulation of Gene Expression ppt
Regulation of Gene Expression pptRegulation of Gene Expression ppt
Regulation of Gene Expression ppt
 
Receptors
ReceptorsReceptors
Receptors
 
Receptor Pharmacology
Receptor PharmacologyReceptor Pharmacology
Receptor Pharmacology
 
Drug receptors in pharmacology
Drug receptors in pharmacologyDrug receptors in pharmacology
Drug receptors in pharmacology
 

Similar to Nuclear receptors and chemical action in cns

Nuclear receptors and chemical action in cns
Nuclear receptors and chemical action in cnsNuclear receptors and chemical action in cns
Nuclear receptors and chemical action in cns
Mustafa Ijaz
 
1. Neurotransmitter-4-BDS.pptx
1. Neurotransmitter-4-BDS.pptx1. Neurotransmitter-4-BDS.pptx
1. Neurotransmitter-4-BDS.pptx
Rajendra Dev Bhatt
 
Chemical transmission and drug action in CNS
Chemical transmission and drug action in CNSChemical transmission and drug action in CNS
Chemical transmission and drug action in CNS
Arslan Tahir
 
CNS PHARMACOLOGY INTRODUCTION - NEUROTRANSMITTERS & MECHANISMS OF DRUG ACTION...
CNS PHARMACOLOGY INTRODUCTION - NEUROTRANSMITTERS & MECHANISMS OF DRUG ACTION...CNS PHARMACOLOGY INTRODUCTION - NEUROTRANSMITTERS & MECHANISMS OF DRUG ACTION...
CNS PHARMACOLOGY INTRODUCTION - NEUROTRANSMITTERS & MECHANISMS OF DRUG ACTION...
Levysikazwe
 
Neurotransmitter 2
Neurotransmitter 2Neurotransmitter 2
Neurotransmitter 2
Bishal Chauhan
 
Neurochemical transmission in the brain dr lateef 2021
Neurochemical transmission in the brain dr lateef 2021Neurochemical transmission in the brain dr lateef 2021
Neurochemical transmission in the brain dr lateef 2021
lateef khan
 
NEUROTRANSMISSION introduction , steps involved
NEUROTRANSMISSION introduction , steps involvedNEUROTRANSMISSION introduction , steps involved
NEUROTRANSMISSION introduction , steps involved
ssuser1c7442
 
Lecture 9- CNS.pptx
Lecture 9- CNS.pptxLecture 9- CNS.pptx
Lecture 9- CNS.pptx
AbdallahAlasal1
 
Noradrenergc transmission
Noradrenergc transmissionNoradrenergc transmission
Noradrenergc transmission
amitgajjar85
 
Noradrenergc transmission
Noradrenergc transmissionNoradrenergc transmission
Noradrenergc transmission
amitgajjar85
 
سلوكية 1
سلوكية 1سلوكية 1
سلوكية 1
mohammedqudairi
 
3- Antipsychotic agents.ppt
3- Antipsychotic agents.ppt3- Antipsychotic agents.ppt
3- Antipsychotic agents.ppt
AshlynnElla3
 
Neurotransmitters ne-ach-histamine by dr.rujul modi
Neurotransmitters   ne-ach-histamine by dr.rujul modiNeurotransmitters   ne-ach-histamine by dr.rujul modi
Neurotransmitters ne-ach-histamine by dr.rujul modi
Rujul Modi
 
PSY-2 Ch03: The Chemistry of Behavior
PSY-2 Ch03: The Chemistry of BehaviorPSY-2 Ch03: The Chemistry of Behavior
PSY-2 Ch03: The Chemistry of Behavior
LauraAdamsPhD
 
Pharmacodynamics.pptx
Pharmacodynamics.pptxPharmacodynamics.pptx
Pharmacodynamics.pptx
Awais irshad
 
Neurohumoral transission in CNS
Neurohumoral transission in CNSNeurohumoral transission in CNS
Neurohumoral transission in CNS
Dekollu Suku
 
Neurotransmitters
NeurotransmittersNeurotransmitters
Neurotransmitters
Ravish Yadav
 
Basic principles of drugs affecting the cns
Basic principles of drugs affecting the cnsBasic principles of drugs affecting the cns
Basic principles of drugs affecting the cns
Dr. Marya Ahsan
 
Neurotransmitters
NeurotransmittersNeurotransmitters
Neurotransmitters
Domina Petric
 
Neurotransmitter
NeurotransmitterNeurotransmitter
Neurotransmitter
Anwar Siddiqui
 

Similar to Nuclear receptors and chemical action in cns (20)

Nuclear receptors and chemical action in cns
Nuclear receptors and chemical action in cnsNuclear receptors and chemical action in cns
Nuclear receptors and chemical action in cns
 
1. Neurotransmitter-4-BDS.pptx
1. Neurotransmitter-4-BDS.pptx1. Neurotransmitter-4-BDS.pptx
1. Neurotransmitter-4-BDS.pptx
 
Chemical transmission and drug action in CNS
Chemical transmission and drug action in CNSChemical transmission and drug action in CNS
Chemical transmission and drug action in CNS
 
CNS PHARMACOLOGY INTRODUCTION - NEUROTRANSMITTERS & MECHANISMS OF DRUG ACTION...
CNS PHARMACOLOGY INTRODUCTION - NEUROTRANSMITTERS & MECHANISMS OF DRUG ACTION...CNS PHARMACOLOGY INTRODUCTION - NEUROTRANSMITTERS & MECHANISMS OF DRUG ACTION...
CNS PHARMACOLOGY INTRODUCTION - NEUROTRANSMITTERS & MECHANISMS OF DRUG ACTION...
 
Neurotransmitter 2
Neurotransmitter 2Neurotransmitter 2
Neurotransmitter 2
 
Neurochemical transmission in the brain dr lateef 2021
Neurochemical transmission in the brain dr lateef 2021Neurochemical transmission in the brain dr lateef 2021
Neurochemical transmission in the brain dr lateef 2021
 
NEUROTRANSMISSION introduction , steps involved
NEUROTRANSMISSION introduction , steps involvedNEUROTRANSMISSION introduction , steps involved
NEUROTRANSMISSION introduction , steps involved
 
Lecture 9- CNS.pptx
Lecture 9- CNS.pptxLecture 9- CNS.pptx
Lecture 9- CNS.pptx
 
Noradrenergc transmission
Noradrenergc transmissionNoradrenergc transmission
Noradrenergc transmission
 
Noradrenergc transmission
Noradrenergc transmissionNoradrenergc transmission
Noradrenergc transmission
 
سلوكية 1
سلوكية 1سلوكية 1
سلوكية 1
 
3- Antipsychotic agents.ppt
3- Antipsychotic agents.ppt3- Antipsychotic agents.ppt
3- Antipsychotic agents.ppt
 
Neurotransmitters ne-ach-histamine by dr.rujul modi
Neurotransmitters   ne-ach-histamine by dr.rujul modiNeurotransmitters   ne-ach-histamine by dr.rujul modi
Neurotransmitters ne-ach-histamine by dr.rujul modi
 
PSY-2 Ch03: The Chemistry of Behavior
PSY-2 Ch03: The Chemistry of BehaviorPSY-2 Ch03: The Chemistry of Behavior
PSY-2 Ch03: The Chemistry of Behavior
 
Pharmacodynamics.pptx
Pharmacodynamics.pptxPharmacodynamics.pptx
Pharmacodynamics.pptx
 
Neurohumoral transission in CNS
Neurohumoral transission in CNSNeurohumoral transission in CNS
Neurohumoral transission in CNS
 
Neurotransmitters
NeurotransmittersNeurotransmitters
Neurotransmitters
 
Basic principles of drugs affecting the cns
Basic principles of drugs affecting the cnsBasic principles of drugs affecting the cns
Basic principles of drugs affecting the cns
 
Neurotransmitters
NeurotransmittersNeurotransmitters
Neurotransmitters
 
Neurotransmitter
NeurotransmitterNeurotransmitter
Neurotransmitter
 

Recently uploaded

share - Lions, tigers, AI and health misinformation, oh my!.pptx
share - Lions, tigers, AI and health misinformation, oh my!.pptxshare - Lions, tigers, AI and health misinformation, oh my!.pptx
share - Lions, tigers, AI and health misinformation, oh my!.pptx
Tina Purnat
 
Histololgy of Female Reproductive System.pptx
Histololgy of Female Reproductive System.pptxHistololgy of Female Reproductive System.pptx
Histololgy of Female Reproductive System.pptx
AyeshaZaid1
 
TEST BANK For Community Health Nursing A Canadian Perspective, 5th Edition by...
TEST BANK For Community Health Nursing A Canadian Perspective, 5th Edition by...TEST BANK For Community Health Nursing A Canadian Perspective, 5th Edition by...
TEST BANK For Community Health Nursing A Canadian Perspective, 5th Edition by...
Donc Test
 
CHEMOTHERAPY_RDP_CHAPTER 6_Anti Malarial Drugs.pdf
CHEMOTHERAPY_RDP_CHAPTER 6_Anti Malarial Drugs.pdfCHEMOTHERAPY_RDP_CHAPTER 6_Anti Malarial Drugs.pdf
CHEMOTHERAPY_RDP_CHAPTER 6_Anti Malarial Drugs.pdf
rishi2789
 
REGULATION FOR COMBINATION PRODUCTS AND MEDICAL DEVICES.pptx
REGULATION FOR COMBINATION PRODUCTS AND MEDICAL DEVICES.pptxREGULATION FOR COMBINATION PRODUCTS AND MEDICAL DEVICES.pptx
REGULATION FOR COMBINATION PRODUCTS AND MEDICAL DEVICES.pptx
LaniyaNasrink
 
How STIs Influence the Development of Pelvic Inflammatory Disease.pptx
How STIs Influence the Development of Pelvic Inflammatory Disease.pptxHow STIs Influence the Development of Pelvic Inflammatory Disease.pptx
How STIs Influence the Development of Pelvic Inflammatory Disease.pptx
FFragrant
 
Top-Vitamin-Supplement-Brands-in-India List
Top-Vitamin-Supplement-Brands-in-India ListTop-Vitamin-Supplement-Brands-in-India List
Top-Vitamin-Supplement-Brands-in-India List
SwisschemDerma
 
The Best Ayurvedic Antacid Tablets in India
The Best Ayurvedic Antacid Tablets in IndiaThe Best Ayurvedic Antacid Tablets in India
The Best Ayurvedic Antacid Tablets in India
Swastik Ayurveda
 
Does Over-Masturbation Contribute to Chronic Prostatitis.pptx
Does Over-Masturbation Contribute to Chronic Prostatitis.pptxDoes Over-Masturbation Contribute to Chronic Prostatitis.pptx
Does Over-Masturbation Contribute to Chronic Prostatitis.pptx
walterHu5
 
Local Advanced Lung Cancer: Artificial Intelligence, Synergetics, Complex Sys...
Local Advanced Lung Cancer: Artificial Intelligence, Synergetics, Complex Sys...Local Advanced Lung Cancer: Artificial Intelligence, Synergetics, Complex Sys...
Local Advanced Lung Cancer: Artificial Intelligence, Synergetics, Complex Sys...
Oleg Kshivets
 
THERAPEUTIC ANTISENSE MOLECULES .pptx
THERAPEUTIC ANTISENSE MOLECULES    .pptxTHERAPEUTIC ANTISENSE MOLECULES    .pptx
THERAPEUTIC ANTISENSE MOLECULES .pptx
70KRISHPATEL
 
Dehradun #ℂall #gIRLS Oyo Hotel 8107221448 #ℂall #gIRL in Dehradun
Dehradun #ℂall #gIRLS Oyo Hotel 8107221448 #ℂall #gIRL in DehradunDehradun #ℂall #gIRLS Oyo Hotel 8107221448 #ℂall #gIRL in Dehradun
Dehradun #ℂall #gIRLS Oyo Hotel 8107221448 #ℂall #gIRL in Dehradun
chandankumarsmartiso
 
8 Surprising Reasons To Meditate 40 Minutes A Day That Can Change Your Life.pptx
8 Surprising Reasons To Meditate 40 Minutes A Day That Can Change Your Life.pptx8 Surprising Reasons To Meditate 40 Minutes A Day That Can Change Your Life.pptx
8 Surprising Reasons To Meditate 40 Minutes A Day That Can Change Your Life.pptx
Holistified Wellness
 
CHEMOTHERAPY_RDP_CHAPTER 2 _LEPROSY.pdf1
CHEMOTHERAPY_RDP_CHAPTER 2 _LEPROSY.pdf1CHEMOTHERAPY_RDP_CHAPTER 2 _LEPROSY.pdf1
CHEMOTHERAPY_RDP_CHAPTER 2 _LEPROSY.pdf1
rishi2789
 
Efficacy of Avartana Sneha in Ayurveda
Efficacy of Avartana Sneha in AyurvedaEfficacy of Avartana Sneha in Ayurveda
Efficacy of Avartana Sneha in Ayurveda
Dr. Jyothirmai Paindla
 
Tests for analysis of different pharmaceutical.pptx
Tests for analysis of different pharmaceutical.pptxTests for analysis of different pharmaceutical.pptx
Tests for analysis of different pharmaceutical.pptx
taiba qazi
 
Adhd Medication Shortage Uk - trinexpharmacy.com
Adhd Medication Shortage Uk - trinexpharmacy.comAdhd Medication Shortage Uk - trinexpharmacy.com
Adhd Medication Shortage Uk - trinexpharmacy.com
reignlana06
 
Journal Article Review on Rasamanikya
Journal Article Review on RasamanikyaJournal Article Review on Rasamanikya
Journal Article Review on Rasamanikya
Dr. Jyothirmai Paindla
 
CHEMOTHERAPY_RDP_CHAPTER 1_ANTI TB DRUGS.pdf
CHEMOTHERAPY_RDP_CHAPTER 1_ANTI TB DRUGS.pdfCHEMOTHERAPY_RDP_CHAPTER 1_ANTI TB DRUGS.pdf
CHEMOTHERAPY_RDP_CHAPTER 1_ANTI TB DRUGS.pdf
rishi2789
 
Novas diretrizes da OMS para os cuidados perinatais de mais qualidade
Novas diretrizes da OMS para os cuidados perinatais de mais qualidadeNovas diretrizes da OMS para os cuidados perinatais de mais qualidade
Novas diretrizes da OMS para os cuidados perinatais de mais qualidade
Prof. Marcus Renato de Carvalho
 

Recently uploaded (20)

share - Lions, tigers, AI and health misinformation, oh my!.pptx
share - Lions, tigers, AI and health misinformation, oh my!.pptxshare - Lions, tigers, AI and health misinformation, oh my!.pptx
share - Lions, tigers, AI and health misinformation, oh my!.pptx
 
Histololgy of Female Reproductive System.pptx
Histololgy of Female Reproductive System.pptxHistololgy of Female Reproductive System.pptx
Histololgy of Female Reproductive System.pptx
 
TEST BANK For Community Health Nursing A Canadian Perspective, 5th Edition by...
TEST BANK For Community Health Nursing A Canadian Perspective, 5th Edition by...TEST BANK For Community Health Nursing A Canadian Perspective, 5th Edition by...
TEST BANK For Community Health Nursing A Canadian Perspective, 5th Edition by...
 
CHEMOTHERAPY_RDP_CHAPTER 6_Anti Malarial Drugs.pdf
CHEMOTHERAPY_RDP_CHAPTER 6_Anti Malarial Drugs.pdfCHEMOTHERAPY_RDP_CHAPTER 6_Anti Malarial Drugs.pdf
CHEMOTHERAPY_RDP_CHAPTER 6_Anti Malarial Drugs.pdf
 
REGULATION FOR COMBINATION PRODUCTS AND MEDICAL DEVICES.pptx
REGULATION FOR COMBINATION PRODUCTS AND MEDICAL DEVICES.pptxREGULATION FOR COMBINATION PRODUCTS AND MEDICAL DEVICES.pptx
REGULATION FOR COMBINATION PRODUCTS AND MEDICAL DEVICES.pptx
 
How STIs Influence the Development of Pelvic Inflammatory Disease.pptx
How STIs Influence the Development of Pelvic Inflammatory Disease.pptxHow STIs Influence the Development of Pelvic Inflammatory Disease.pptx
How STIs Influence the Development of Pelvic Inflammatory Disease.pptx
 
Top-Vitamin-Supplement-Brands-in-India List
Top-Vitamin-Supplement-Brands-in-India ListTop-Vitamin-Supplement-Brands-in-India List
Top-Vitamin-Supplement-Brands-in-India List
 
The Best Ayurvedic Antacid Tablets in India
The Best Ayurvedic Antacid Tablets in IndiaThe Best Ayurvedic Antacid Tablets in India
The Best Ayurvedic Antacid Tablets in India
 
Does Over-Masturbation Contribute to Chronic Prostatitis.pptx
Does Over-Masturbation Contribute to Chronic Prostatitis.pptxDoes Over-Masturbation Contribute to Chronic Prostatitis.pptx
Does Over-Masturbation Contribute to Chronic Prostatitis.pptx
 
Local Advanced Lung Cancer: Artificial Intelligence, Synergetics, Complex Sys...
Local Advanced Lung Cancer: Artificial Intelligence, Synergetics, Complex Sys...Local Advanced Lung Cancer: Artificial Intelligence, Synergetics, Complex Sys...
Local Advanced Lung Cancer: Artificial Intelligence, Synergetics, Complex Sys...
 
THERAPEUTIC ANTISENSE MOLECULES .pptx
THERAPEUTIC ANTISENSE MOLECULES    .pptxTHERAPEUTIC ANTISENSE MOLECULES    .pptx
THERAPEUTIC ANTISENSE MOLECULES .pptx
 
Dehradun #ℂall #gIRLS Oyo Hotel 8107221448 #ℂall #gIRL in Dehradun
Dehradun #ℂall #gIRLS Oyo Hotel 8107221448 #ℂall #gIRL in DehradunDehradun #ℂall #gIRLS Oyo Hotel 8107221448 #ℂall #gIRL in Dehradun
Dehradun #ℂall #gIRLS Oyo Hotel 8107221448 #ℂall #gIRL in Dehradun
 
8 Surprising Reasons To Meditate 40 Minutes A Day That Can Change Your Life.pptx
8 Surprising Reasons To Meditate 40 Minutes A Day That Can Change Your Life.pptx8 Surprising Reasons To Meditate 40 Minutes A Day That Can Change Your Life.pptx
8 Surprising Reasons To Meditate 40 Minutes A Day That Can Change Your Life.pptx
 
CHEMOTHERAPY_RDP_CHAPTER 2 _LEPROSY.pdf1
CHEMOTHERAPY_RDP_CHAPTER 2 _LEPROSY.pdf1CHEMOTHERAPY_RDP_CHAPTER 2 _LEPROSY.pdf1
CHEMOTHERAPY_RDP_CHAPTER 2 _LEPROSY.pdf1
 
Efficacy of Avartana Sneha in Ayurveda
Efficacy of Avartana Sneha in AyurvedaEfficacy of Avartana Sneha in Ayurveda
Efficacy of Avartana Sneha in Ayurveda
 
Tests for analysis of different pharmaceutical.pptx
Tests for analysis of different pharmaceutical.pptxTests for analysis of different pharmaceutical.pptx
Tests for analysis of different pharmaceutical.pptx
 
Adhd Medication Shortage Uk - trinexpharmacy.com
Adhd Medication Shortage Uk - trinexpharmacy.comAdhd Medication Shortage Uk - trinexpharmacy.com
Adhd Medication Shortage Uk - trinexpharmacy.com
 
Journal Article Review on Rasamanikya
Journal Article Review on RasamanikyaJournal Article Review on Rasamanikya
Journal Article Review on Rasamanikya
 
CHEMOTHERAPY_RDP_CHAPTER 1_ANTI TB DRUGS.pdf
CHEMOTHERAPY_RDP_CHAPTER 1_ANTI TB DRUGS.pdfCHEMOTHERAPY_RDP_CHAPTER 1_ANTI TB DRUGS.pdf
CHEMOTHERAPY_RDP_CHAPTER 1_ANTI TB DRUGS.pdf
 
Novas diretrizes da OMS para os cuidados perinatais de mais qualidade
Novas diretrizes da OMS para os cuidados perinatais de mais qualidadeNovas diretrizes da OMS para os cuidados perinatais de mais qualidade
Novas diretrizes da OMS para os cuidados perinatais de mais qualidade
 

Nuclear receptors and chemical action in cns

  • 1.
  • 2. NUCLEAR RECEPTOS & CHEMICAL TRANSMISSION AND DRUG ACTION IN THE CNS Introduction Structure Mechanism of Action Classification of Psychotropic Drug Targets for Drugs Action Drug in CNS
  • 3. NUCLEAR RECEPTORS “Nuclear receptors are a family of highly conserved transcription in response to small lipophilic compound.” Play important role in development, physiology and disease in humans by regulating gene expression (Protein or amino acid formation) Estrogen or β-estradiol act upon the nuclear receptor to regulate gene expression for Female Sex Development Testosterone or Androgens act upon nuclear receptors to regulate gene expression for Male Sex Development
  • 4. STRUCTURE All nuclear are monomeric proteins Share broadly similar structural design It has six domains (A-F): (A-B) N-regulatory domain (C) DNA binding domain (D) Hinge Region (E) Ligand binding domain (F) C-terminal domain
  • 5. STRUCTURE (A-B) N-regulatory domain: Highly variable in sequence between various nuclear receptors (C) DNA binding domain: Highly conserved, contain two zinc fingers that bind to specific DNA sequences (D) Hinge Region: Flexible domain (E) Ligand binding domain: it is alpha helical sandwich fold, three anti-parallel helices flanked by two alpha helices on one side and three on the other, binding cavity is within the inferior of the LBD and just below three anti-parallel alpha helical sandwich (F) C-terminal domain: Highly variable sequence, Near to it are located the motifs that contain nuclear localization signals
  • 6.
  • 7. FUNCTIONS OF THE DOMAINS N-terminal domain: harbors AF1 site that binds to other cell specific transcription factors in a ligand-independent way and modifies the binding or activity of the receptor DNA binding domain: Binds to the specific sequences of DNA called hormone response element Hinge region: Connects the DNA binding domain to the ligand binding domain Ligand binding domain: Harbors the AF2 whose action depends upon the bound ligand C-terminal domain: has ability to the transcription
  • 8. MECHANISM OF ACTION Classes Class I nuclear receptors Class II nuclear receptors Class III nuclear receptors
  • 9. MECHANISM OF ACTION Class I Nuclear Receptors: Largely steroid receptors Ligands are mainly steroids Located in cytoplasm or attached to cytoskeleton or other structures When ligand binds, form homodimers in the presence of their partners and migrate to nucleus to trigger signal response A single ligand can regulate a large number of genes
  • 10. MECHANISM OF ACTION Class II Nuclear Receptors: Their ligands are mainly lipids Located in nucleus They form heterodimers with retinoid X receptors Class III Nuclear Receptors: They transduce endocrine signals but function as heterodimers
  • 11.
  • 12. CHEMICAL TRANSMISSION AND DRUG ACTION IN THE CNS
  • 13. INTRODUCTION • Drugs acting on CNS are of special significance and of major therapeutic use but also the drugs which are commonly administered for non-medical reasons like coffee, tea and nicotine • CNS is functionally more complex. Behavior of drug on the individual cell of brain is different from the whole brain unlike the other organs Two reasons for understanding the action of drugs on CNS is difficult:
  • 14. CHEMICAL SIGNALING IN THE CNS CNS produce neurotransmitter which start processes in the body and control the biological functions It is important to study the physiology of brain and to study chemical signaling because whole body is linked with it. Drug acting upon CNS will also produce effects on the body. For Example,
  • 15. Adrenaline, controls the eyes and little bit dryness of mouth Dopamine, disturbance in its release leads to Parkinson’s disease GABA, is related to anxiety CHEMICAL SIGNALING IN THE CNS
  • 16. CHEMICAL SIGNALING IN THE CNS Neurotransmitters control various process in the body in a range of different time scales. The time scale may be in Miliseconds Minutes Hours Days Months Year Brain system works like a candy floss into the grand canyon Candy floss mean number of threads that are placed on a stick and enter into a grand canyon
  • 17.
  • 18. TARGETS FOR DRUG ACTION Targets for drug action Receptors Enzymes Ion channels Carrier Molecules
  • 19. Receptors • A protein that recognizes the body’s natural mediator or the drug • When ligand will bind, it transmits signal and elicits a biological effect Ion channels • Ion channels are proteins in membrane that allow passage of specific ions only when activated • Upon receiving signals, it will open and allows the ions to pass Enzymes • Biological catalysts that speed up chemical reaction without being changed • Many drugs act by inhibiting the action of enzymes Carrier molecules • Membrane bounded proteins that transport specific molecules • Molecule to be transported binds to specific protein for recognition site on the carrier and then molecule is transferred to other side of membrane TARGETS FOR DRUG ACTION
  • 20. DRUG ACTION IN CNS Study action of drug on brain is difficult due to complexity of neuronal interconnections in the brain Difficult to predict effects of blocking or enhancing release or action of one or other neurotransmitters greatly depend upon External inputs Influence of glial cells Range of secondary adaptive responses Blood brain barrier
  • 21.
  • 22. Drug transport to specific target in brain Direct penetration Small non-polar molecules diffuse passively across cell membrane Penetration via transporters Transporters facilitate entry into brain DRUG ACTION IN CNS
  • 23. CLASSIFICATION OF PSYCHOTROPIC DRUGS Anaesthetic agents • Used to produce surgical anesthesia • For example, halothane, propofol Anxiolytic and Sedatives • Used to induce sleep and reduce anxiety • Hypnotics, sedatives, minor tranquilizers • For example, barbiturates, benzodiazepines Antipyschoti cs drugs • Used to relieve schizophrenic illness • Neuroleptics, major tranquilizers • Clozapine, chlorpronazine Antidepressa nt drugs • Used to relieve depressive illness • Thymoleptics • Escitalopram
  • 24. Analgesic drugs • Used to relieve from pain • For example, opiates and carbamazepine Psychomotor stimulants • Used to induce wakefulness and euphoria • Psychostimulants • For example, amphetamine, cocaine, caffeine Psychotomimetic drugs • Used to cause disturbance of perception • Hallucinogens, psychodysleptics • For example, mesacline, phencyclidine Cognition enhancers • Used to improve memory and cognitive performance • Nootropic drugs • For example, tacrine, donepezil CLASSIFICATION OF PSYCHOTROPIC DRUGS
  • 25. Some drugs defy this classification For example, lithium, dissociative anesthetic, used in the treatment of manic depressive psychosis and ketamine It produces psychotropic effect rather similar to those produced by phecyclidine CLASSIFICATION OF PSYCHOTROPIC DRUGS