Definition
Classification and description of each class.
Description of individual receptor.
Forces affecting the drug receptor binding.
Binding of drug receptor affect drug action.
Agonist and antagonist.
Disease due to malfunctioning of receptors.
New drug design based on structure of receptors
Receptor as target for drug discovery.
Drug action not mediated by receptor.
Definition
Classification and description of each class.
Description of individual receptor.
Forces affecting the drug receptor binding.
Binding of drug receptor affect drug action.
Agonist and antagonist.
Disease due to malfunctioning of receptors.
New drug design based on structure of receptors
Receptor as target for drug discovery.
Drug action not mediated by receptor.
Neurotransmission (Latin: transmission "passage, crossing" from transmitter "send, let through"), is the process by which signalling molecules called neurotransmitters are released by the axon terminal of a neuron and bind to and react with the receptors on the dendrites of another neuron
GPCRs are the most dynamic and most abundant all the receptors. The G protein-coupled receptor (GPCR) superfamily comprises the largest and most diverse group of proteins in mammals. GPCRs are responsible for every aspect of human biology from vision, taste, sense of smell, sympathetic and parasympathetic nervous functions, metabolism, and immune regulation to reproduction. GPCRs interact with a number of ligands ranging from photons, ions, amino acids, odorants, pheromones, eicosanoids, neurotransmitters, peptides, proteins, and hormones.
Nevertheless, for the majority of GPCRs, the identity of their natural ligands is still unknown, hence remain orphan receptors.
The simple dogma that underpins much of our current understanding of GPCRs, namely,
one GPCR gene− one GPCR protein− one functional GPCR− one G protein −one response
is showing distinct signs of wear.
Classification of receptors family by vivek sharmaAnimatedWorld
Definition- Receptor are the biologic molecule to which drug bind and produces a measurable response.
So, enzyme and structural proteins can be considerd to be pharmacologic receptors.
Majorly receptor are of 4 types and the molecule or a drug interact to receptor to give response often called as ligand.
The type of receptor a ligand will bind is depend on the nature of ligand.
Hydrophilliic ligand binds to the receptor found on the cell surface.
Hydrophobic ligand can enter the cell membrane to intract the receptor present on inside the cells.
Classification of Receptors
A. Cell surface receptor
Ligand-gated Ion Channel
G Protein Coupled Receptor
Enzyme linked Receptor
B. Intracellular Receptor
Nuclear Receptor
My presentation on neurotransmitter glutamate. References from Comprehensive textbook of psychiatry 9th edition and Stahl's essential psychopharmacology 4th edition.
This presentation impart a knowledge about Histamine,receptor,and antagonist.
Recent advances also mentioned like H3 & H4 receptors role in cognitive impairment etc.
Neurotransmission (Latin: transmission "passage, crossing" from transmitter "send, let through"), is the process by which signalling molecules called neurotransmitters are released by the axon terminal of a neuron and bind to and react with the receptors on the dendrites of another neuron
GPCRs are the most dynamic and most abundant all the receptors. The G protein-coupled receptor (GPCR) superfamily comprises the largest and most diverse group of proteins in mammals. GPCRs are responsible for every aspect of human biology from vision, taste, sense of smell, sympathetic and parasympathetic nervous functions, metabolism, and immune regulation to reproduction. GPCRs interact with a number of ligands ranging from photons, ions, amino acids, odorants, pheromones, eicosanoids, neurotransmitters, peptides, proteins, and hormones.
Nevertheless, for the majority of GPCRs, the identity of their natural ligands is still unknown, hence remain orphan receptors.
The simple dogma that underpins much of our current understanding of GPCRs, namely,
one GPCR gene− one GPCR protein− one functional GPCR− one G protein −one response
is showing distinct signs of wear.
Classification of receptors family by vivek sharmaAnimatedWorld
Definition- Receptor are the biologic molecule to which drug bind and produces a measurable response.
So, enzyme and structural proteins can be considerd to be pharmacologic receptors.
Majorly receptor are of 4 types and the molecule or a drug interact to receptor to give response often called as ligand.
The type of receptor a ligand will bind is depend on the nature of ligand.
Hydrophilliic ligand binds to the receptor found on the cell surface.
Hydrophobic ligand can enter the cell membrane to intract the receptor present on inside the cells.
Classification of Receptors
A. Cell surface receptor
Ligand-gated Ion Channel
G Protein Coupled Receptor
Enzyme linked Receptor
B. Intracellular Receptor
Nuclear Receptor
My presentation on neurotransmitter glutamate. References from Comprehensive textbook of psychiatry 9th edition and Stahl's essential psychopharmacology 4th edition.
This presentation impart a knowledge about Histamine,receptor,and antagonist.
Recent advances also mentioned like H3 & H4 receptors role in cognitive impairment etc.
Signal transduction in plant defense responsesVINOD BARPA
Signal transduction a Process by which a cell converts one kind of signal into another. Plant disease resistance and susceptibility are gov¬erned by the combined genotypes of host and pathogen and depend on a complex exchange of signals and responses occurring under given environmental con¬ditions. During the long process of host-pathogen co-evolution, plants have developed various elaborate mechanisms to ward off pathogen attack. Whereas some of these defense mechanisms are preformed and provide physical and chemical barriers to hinder pathogen infection, others are induced only after pa¬thogen attack. Similar to animal immune responses, induced plant defense responses involve a network of signal transduction and the rapid activation of gene expression following pathogen infection. They do not have immune system and locomotary organs to escape environmental challenges and biotic stresses. In plant, nature has provided them some preformed and inducible defense resistance. Host recognition of invading pathogen is often determined by the so called “gene for gene” interaction between avirulence (avr) gene of pathogen and corresponding resistance (R) gene of host (Flor, 1971) which encode receptor for the recognition of specific elicitor or ligand encoded directly or indirectly by pathogen avr gene. Recent studies have revealed intriguing parallels between animal and plant defense responses as demonstrated by the structural and functional conservation of some of their signal transduction processes. Furthermore, signaling components such as G proteins, NADPH oxidase, H202, salicylic acid (SA, and aspirin), mitogen-activated protein kinases (MAPK), and transcription factors have been shown to be associated with or participate in both animal and plant defense responses, suggesting the presence of con¬served signaling pathways for host defenses in diverse higher eukaryotes.
A receptor is a protein molecule usually found embedded within the plasma membrane surface of a cell that receives chemical signals from outside the cell and when such chemical signals bind to a receptor, they cause some form of cellular/tissue response.
Receptor is a macromolecule whose function is to recognize and respond to chemical signal
There are 3 types of receptors. Those are:
i. Internal /Intracellular/Cytoplasmic receptors:
found in the cytoplasm of the cell
respond to hydrophobic ligand molecules
ii. Cell-surface / transmembrane receptors/ cell specific proteins
performs signal transduction, converting an extracellular signal into an intracellular signal.
iii. Nuclear receptor
Located in the nucleus of the cell
i. Internal /Intracellular/Cytoplasmic receptors
Steriod receptor
ii. Cell-surface / transmembrane receptors/ cell specific proteins
G-protein- coupled receptor
Enzyme- linked receptor/ tyrosin kinase receptor
Ion channel- linked receptor/ ligand gated receptor
iii. Nuclear receptor
Thyroid receptor
Introduction to chromatography, Definition of Chromatography, Types of column chromatography, Theory of chromatography, Practical considerations in column chromatography , Factors affecting efficiency of a column, Applications.
ANTI - INFLAMMATORY ACTIVITY OF LEAVES OF JATROPHA GOSSYPIFOLIA L.Raju Sanghvi
BY HRBC MEMBRANE STABILIZATION METHOD, Introduction, Preparation of extracts, Chemicals and instruments, In vitro anti – inflammatory activity, Acute oral toxicity study, Discussion
Introduction & Definition, Theory, instrumentation, Continuous – wave (CW) instrument, The pulsed Fourier Transform [FT] instrument, Solvents, Chemical shift
i. Shielding and de-shielding
ii. Factors affecting chemical shift
How to Split Bills in the Odoo 17 POS ModuleCeline George
Bills have a main role in point of sale procedure. It will help to track sales, handling payments and giving receipts to customers. Bill splitting also has an important role in POS. For example, If some friends come together for dinner and if they want to divide the bill then it is possible by POS bill splitting. This slide will show how to split bills in odoo 17 POS.
How to Make a Field invisible in Odoo 17Celine George
It is possible to hide or invisible some fields in odoo. Commonly using “invisible” attribute in the field definition to invisible the fields. This slide will show how to make a field invisible in odoo 17.
The French Revolution, which began in 1789, was a period of radical social and political upheaval in France. It marked the decline of absolute monarchies, the rise of secular and democratic republics, and the eventual rise of Napoleon Bonaparte. This revolutionary period is crucial in understanding the transition from feudalism to modernity in Europe.
For more information, visit-www.vavaclasses.com
The Roman Empire A Historical Colossus.pdfkaushalkr1407
The Roman Empire, a vast and enduring power, stands as one of history's most remarkable civilizations, leaving an indelible imprint on the world. It emerged from the Roman Republic, transitioning into an imperial powerhouse under the leadership of Augustus Caesar in 27 BCE. This transformation marked the beginning of an era defined by unprecedented territorial expansion, architectural marvels, and profound cultural influence.
The empire's roots lie in the city of Rome, founded, according to legend, by Romulus in 753 BCE. Over centuries, Rome evolved from a small settlement to a formidable republic, characterized by a complex political system with elected officials and checks on power. However, internal strife, class conflicts, and military ambitions paved the way for the end of the Republic. Julius Caesar’s dictatorship and subsequent assassination in 44 BCE created a power vacuum, leading to a civil war. Octavian, later Augustus, emerged victorious, heralding the Roman Empire’s birth.
Under Augustus, the empire experienced the Pax Romana, a 200-year period of relative peace and stability. Augustus reformed the military, established efficient administrative systems, and initiated grand construction projects. The empire's borders expanded, encompassing territories from Britain to Egypt and from Spain to the Euphrates. Roman legions, renowned for their discipline and engineering prowess, secured and maintained these vast territories, building roads, fortifications, and cities that facilitated control and integration.
The Roman Empire’s society was hierarchical, with a rigid class system. At the top were the patricians, wealthy elites who held significant political power. Below them were the plebeians, free citizens with limited political influence, and the vast numbers of slaves who formed the backbone of the economy. The family unit was central, governed by the paterfamilias, the male head who held absolute authority.
Culturally, the Romans were eclectic, absorbing and adapting elements from the civilizations they encountered, particularly the Greeks. Roman art, literature, and philosophy reflected this synthesis, creating a rich cultural tapestry. Latin, the Roman language, became the lingua franca of the Western world, influencing numerous modern languages.
Roman architecture and engineering achievements were monumental. They perfected the arch, vault, and dome, constructing enduring structures like the Colosseum, Pantheon, and aqueducts. These engineering marvels not only showcased Roman ingenuity but also served practical purposes, from public entertainment to water supply.
The Art Pastor's Guide to Sabbath | Steve ThomasonSteve Thomason
What is the purpose of the Sabbath Law in the Torah. It is interesting to compare how the context of the law shifts from Exodus to Deuteronomy. Who gets to rest, and why?
This is a presentation by Dada Robert in a Your Skill Boost masterclass organised by the Excellence Foundation for South Sudan (EFSS) on Saturday, the 25th and Sunday, the 26th of May 2024.
He discussed the concept of quality improvement, emphasizing its applicability to various aspects of life, including personal, project, and program improvements. He defined quality as doing the right thing at the right time in the right way to achieve the best possible results and discussed the concept of the "gap" between what we know and what we do, and how this gap represents the areas we need to improve. He explained the scientific approach to quality improvement, which involves systematic performance analysis, testing and learning, and implementing change ideas. He also highlighted the importance of client focus and a team approach to quality improvement.
Welcome to TechSoup New Member Orientation and Q&A (May 2024).pdfTechSoup
In this webinar you will learn how your organization can access TechSoup's wide variety of product discount and donation programs. From hardware to software, we'll give you a tour of the tools available to help your nonprofit with productivity, collaboration, financial management, donor tracking, security, and more.
How to Create Map Views in the Odoo 17 ERPCeline George
The map views are useful for providing a geographical representation of data. They allow users to visualize and analyze the data in a more intuitive manner.
1. RECEPTORS
Presented by
VENKAT SANNAPU(11AB1R0057)
Under the guidance of
Mrs.B.DEEPTHI M.Pharm (PhD)
VIGNAN PHARMACY COLLEGE
(Affiliated to JNTU Kakinada Approved by PCI & AICTE, New Delhi)
Vadlamudi , Guntur, Andhra Pradesh
2. CONTENTS
Introduction - receptor
Drug – receptor interactions
Ligand gated ion channel receptors
G – protein coupled receptors
Kinase liked receptors
Nuclear receptors
Comparison of receptor types
Conclusion
References
RECEPTORS @ VPC
2
3. WHAT IS A RECEPTOR?
o Specialized areas of cell to which drugs get bound.
They are regulatory protein macro molecules .
Drug should have –selectivity to a receptor ; receptor should have
ligand specificity to elicit action.
RECEPTORS @ VPC
3
4. DRUG RECEPTOR INTERACTIONS
Effect of drug attributed to two factors
1. Affinity : tendency of the drug to bind to receptor and form D-R
complex .
2. Efficacy or intrinsic activity : ability of the drug to trigger
pharmacological responses after forming D-R complex .
RECEPTORS @ VPC
4
5. CONTD…
Based on affinity and intrinsic activity :
Full agonist : high affinity
high intrinsic activity(=1)
Eg. Methacholine on acetylcholine receptors
Antagonist : only affinity
no intrinsic activity (=0)
Eg. Atropine on muscarinic receptors
RECEPTORS @ VPC
5
8. Also called ionotropic receptors.
Involved mainly in fast synaptic transmission.
RECEPTORS @ VPC
Eg: nAchR, GABAA, and glutamate receptors of the NMDA, AMPA and
kainate types.
8
9. FEATURES – ION CHANNELS
Protein molecules form water filled
pores that span the membrane.
Switch between open and closed states.
RECEPTORS @ VPC
Rate and Direction of movement depends on electrochemical gradient of
the ions
9
10. MOLECULAR STRUCTURE
ligand binding site in extracellular domain.
4 subunits α, β, γ and δ.
α2, β, γ - pentameric str - 2 ligand binding sites
RECEPTORS @ VPC
Each subunit spans the membrane 4 times; all subunits form a central
pore.
10
15. CONTD…
Due to the concentration changes of different ions the following effects are
seen.
Increase in Na+ and Ca+ levels- excitatory
Decrease in Na+ and Ca+ levels- inhibitory
Increase in K+ levels – inhibitory
Decrease in K+ levels – excitatory
Increase in Cl- levels – inhibitory
Decrease in Cl- levels- excitatory
RECEPTORS @ VPC
15
16. ION CHANNELS - IMPORTANCE
Generation , propagation of nerve impulse.
Synaptic transmission of neurons.
Muscle contraction.
Salt balance.
Hormone release.
RECEPTORS @ VPC
16
Muscle relaxants , anti-arrhythmatics ,anesthetics – act by blocking ion channels.
17. metabotropic or 7-transmembrane-spanning (heptahelical) receptors.
coupled to intracellular effector systems via a G-protein.
RECEPTORS @ VPC
mAChRs, adrenoceptors, dopamine, 5-HT, opiate, peptide, purinoceptors,
orphans .
17
22. G-PROTEIN RECEPTOR FOR SIGNALLING PATHWAY
GO NT ,Opioid
cannabinoid
Not clear
Gq mAchR, serotonin
5HT1C
PLC
IP3 , DAG
Cytoplasmic Ca
Gt1 , Gt2 Rhodopsin and colour
opsins in retinal rod
and cone cells
cGMP
phosphodiesterase-cGMP
RECEPTORS @ VPC
22
23. SECONDARY MESSENGER SYSTEMS INVOLVED IN SIGNAL
TRANSDUCTION
The adenyly cyclase / cAMP system
The Phospholipase C / inositol phosphate system
The Ion channels
The Rho A /Rho kinase system
RECEPTORS @ VPC
23
24. ADENYLYL CYCLASE/ CAMP SYSTEM
c AMP –nucleotide synthesized from ATP - by adenylyl cyclase,
metabolized by PDE.
Regulate enzymes of metabolism, growth, contractile proteins of muscle.
NT - acts on GPCR –Gs/Gi activated - produce effects – by inc or dec.
activity of adenylyl cylase-and cAMP.
c AMP- activate - Protein kinases-activate/inactivate enzymes by
phosphorylation – cellular events.
RECEPTORS @ VPC
24
25. PHOSPHOLIPASE C-INOSITOL SYSTEM
Phospholipase C : Cleaves membrane phospholipids - phosphoinositides.
PLC beta – cleaves phosphatidylinositol(4,5)bis Phosphate PIP2 - into DAG
and IP3.
DAG and IP3 - Secondary messenegers – elicit cellular responses.
RECEPTORS @ VPC
25
26. ION CHANNELS
GPCR- directly control ion channel-without secondary messenger.
Eg. mAchR in heart – activate K+ channel.
RECEPTORS @ VPC
26
27. Involved in growth, proliferation, differentiation or survival-called growth
factors.
Mediate actions of protein mediators- GF, cytokines , harmones - insulin and
leptin.
Slow – require the expression of new genes.
Single membrane spanning helix - extracellular ligand binding domain -
intracellular domain.
RECEPTORS @ VPC
27
28. Structure of Kinases linked receptors
Y
Y
Y
Y
Y
Y
Extracellular domain
Binds to the ligand (growth factor)
Trans membrane domain
Intracellular domain
Endogenous kinases bind
and get phosphorlated
RECEPTORS @ VPC
28
31. Important pathways activated :
1. The Ras/Raf/mitogen- activated protein (MAP) kinase pathway
- activated by tyrosine kinases.
- important in cell division, growth, differentiation.
2. The Jak/Stat pathway
- activated by cytokines.
-controls synthesis and release of inflammatory mediators.
RECEPTORS @ VPC
31
32. Ligand activated transcription factors.
Present in soluble form – either in cytoplasm or nucleus – freely diffusable.
Transduce signals by- modifying gene transcription.
Eg: steroid hormones, glucocorticoids, vit D and A, orphan receptors
Play vital role in endocrine signaling and metabolic regulation.
RECEPTORS @ VPC
32
33. Zn fingers;hor
response elements
-Binds with corepressor
coactivator ptns
AF1
AF2
RECEPTORS @ VPC
33
34. CONCLUSION
Extensive research done on Receptor pharmacology -lead to discovery of
new drug targets for treatment of several diseases.
Still requires discovery of new receptor types and the mechanisms of many
orphan receptors that can result in effective treatment of many diseases.
Requires development of receptor crystallization etc.
Much to be discovered about the nuclear receptors.
RECEPTORS @ VPC
34
35. ACKNOWLEDGEMENT
I would like to thank my guide, Mrs. B. Deepthi for her
constant guidance and support .
I would also like to thank our principal, Mr. P. Srinivasa
Babu and the seminar committee for giving me this
opportunity.
RECEPTORS @ VPC
35
36. REFERENCES
Rang , Dale, Ritter ,Flower :Rang and Dale’s,
pharmacology;6th edition, Churchill Livingstone;2008,
9-52.
Bertram G. Katzung , Basic and clinical pharmacology;
10th edition ; 2006 , 197-209
KD Tripati , essentials of medical pharmacology ; 6th
edition; 2008, 40-52.
RICHARD’s LIPPINCOTT’s illustrated reviews of
PHARMACOLOGY , 4th edition , Page no 25 – 34.
RECEPTORS @ VPC
36