This document discusses ion channels, which are pore-forming membrane proteins that control the flow of ions across cell membranes. There are two main classes of ion channels: voltage-gated channels, whose gating is controlled by membrane polarization, and ligand-gated channels, whose gating is controlled by the binding of intracellular ligands. The document provides examples of different types of ion channels including potassium channels, calcium channels, chloride channels, GABA and glycine receptors. It also discusses some drugs that work by blocking specific ion channels and their potential applications.
1. ION CHANNELS
2. ION CHANNEL RECEPTORS- PRINCIPLES
3. STRUCTURE OF ION CHANNEL RECEPTORS
4. VOLTAGE GATED ION CHANNELS
5. LIGAND GATED ION CHANNELS
6. THANKS
Receptor types, mechanism, receptor pharmacology, drug receptor interactions, theories of receptor pharmacology, spare receptors and new concepts like biased agonism
cellular level understanding of potassium channels, molecular levels, K+ channels, drugs on potassium channels, transmission of potassium across membrane, cell transport system, types of potassium channels, voltage gated, ligand gated, tandem pore
Ion channels, types and their importace in managment of diseasesFarazaJaved
This topic covers voltage gated type of ion channel, general structure and functioning of ion channels and involvement of different ion channel types in the pathogenesis as wella as a target for the development of various diseases.
1. ION CHANNELS
2. ION CHANNEL RECEPTORS- PRINCIPLES
3. STRUCTURE OF ION CHANNEL RECEPTORS
4. VOLTAGE GATED ION CHANNELS
5. LIGAND GATED ION CHANNELS
6. THANKS
Receptor types, mechanism, receptor pharmacology, drug receptor interactions, theories of receptor pharmacology, spare receptors and new concepts like biased agonism
cellular level understanding of potassium channels, molecular levels, K+ channels, drugs on potassium channels, transmission of potassium across membrane, cell transport system, types of potassium channels, voltage gated, ligand gated, tandem pore
Ion channels, types and their importace in managment of diseasesFarazaJaved
This topic covers voltage gated type of ion channel, general structure and functioning of ion channels and involvement of different ion channel types in the pathogenesis as wella as a target for the development of various diseases.
DRUGS AFFECTING THE SODIUM CHANNEL BOTH BLOCKER AND OPENERS, STRUCTURE OF SODIUM CHANNEL AND ITS LOCATION. SODIUM CHANNEL GATTING MECHANISM BY WITCH THEY ACTING. TYPES OF SODIUM CHANNEL AND ITS FUCTIONS. THEIR THERAPEUTIC APPLICATION WITH EXAMPLES OF DRUGS.
This slides were prepared for My Post Graduation activities and seminar most of them are from sources such as slide share, Pub Med, Standard Pharmacology Textbooks ....
Feel free to comment/correct/suggest Thank you
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
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
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.
Introduction to Immunotherapeutics
Cell mediated & humoral immunity, Immunosuppressants, Immunostimulants
Presented by
G. Sai Swetha
Department of Pharmacology
DRUGS AFFECTING THE SODIUM CHANNEL BOTH BLOCKER AND OPENERS, STRUCTURE OF SODIUM CHANNEL AND ITS LOCATION. SODIUM CHANNEL GATTING MECHANISM BY WITCH THEY ACTING. TYPES OF SODIUM CHANNEL AND ITS FUCTIONS. THEIR THERAPEUTIC APPLICATION WITH EXAMPLES OF DRUGS.
This slides were prepared for My Post Graduation activities and seminar most of them are from sources such as slide share, Pub Med, Standard Pharmacology Textbooks ....
Feel free to comment/correct/suggest Thank you
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
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
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.
Introduction to Immunotherapeutics
Cell mediated & humoral immunity, Immunosuppressants, Immunostimulants
Presented by
G. Sai Swetha
Department of Pharmacology
روش های تصمیم گیری چند معیاره
anp / topsis / electre / vikor / promethee / demital / saw / oreste / gra / sir / bwm / ....
شرح روش ها همراه با مثال های کار بردی و نتیجه گیری در اخر کار
Day 4-TRANSPORT ACROSS THE CELL MEMBRANE (5)b.pptxMkindi Mkindi
There are nearly 100 viruses of the herpes group that infect many different animal species.
Official name of herpesviruses that commonly infect human is Humans herpesvirus (HHV)
herpes simplex virus types 1 (HHV 1)
Herpes simplex virus type 2 (HHV 2)
Varicella-zoster virus (HHV 3)
Epstein-Barr virus, (HHV 4)
Cytomegalovirus (HHV 5)
Human herpesvirus 6 (HHV 6)
Human herpesvirus 7 (HHV 7)
Human herpesvirus 8 (HHV 8) (Kaposi's sarcoma-associated herpesvirus).
Herpes B virus of monkeys can also infect humans
hELMINTHS#corona virus#Aspergillosis#BUGANDO#CUHAS#CUHAS#CUHAS#CELL MEMBRANE TRANSPORT#PHYSIOLOGY#BODY FLUIDS#RENAL PHYSIOLOGY#
Individualized Webcam facilitated and e-Classroom USMLE Step 1 Tutorials with Dr. Cray. 1 BMS Unit is 4 hr. General Principles and some Organ System require multiple units to complete in preparation for the USMLE Step 1 A HIGH YIELD FOCUS IN Biochemistry / Cell Biology, Microbiology / Immunology and the 4 P’s-Phiso, Pathophys, Path and Pharm. Webcam Facilitated USMLE Step 2 Clinical Knowledge and Clinical Skills diadactic tutorials /1 Unit is 4 hours, individualized one-on-one and group sessions, Including all Internal Medicine sub-sub-specitialities. For questions or more information.. drcray@imhotepvirtualmedsch.com
The generation of an action potential in heart muscle
cells depends on the opening and closing of ionselective channels in the plasma membrane.
The patch-clamp technique enables the investigation of
drug interactions with ion-channel .
The Isolated cells are ready for experiment.
Glass micro-pipette - a tip opening of about 1 μm, is
placed onto the cell
3. Ion channels are pore-forming membrane
proteins whose functions include establishing
a resting membrane potential, shaping action
potentials and other electrical signals
by gating the flow of ions across the cell
membrane, controlling the flow of ions
across secretory and epithelial cells, and
regulating cell volume
4. Schematic diagram of an
ion channel
1 -channel domains(typically
four per channel), 2 - outer
vestibule, 3 - selectivity
filter, 4 - diameter of
selectivity filter, 5 -
phosphorylation site, 6 -cell
membrane.
5. Ion channels are considered to be one of the
two traditional classes of ionophoric
proteins, with the other class known as ion
transporters (including the sodium-potassium
pump, sodium-calcium exchanger,
and sodium-glucose transport proteins,
amongst others)
Potassium channels form most abundant &
diverse class of ion channels
6. Study of ion channels (channelomics) often includes
biophysics, electrophysiology & pharmacology,
utilizing techniques including voltage clamp, patch
clamp, immunohistochemistry, X-ray fluorescence,
and RT-PCR.
7. There are two distinctive features of ion channels that
differentiate them from other types of ion transporter
proteins:
The rate of ion transport through the channel is
very high (often 106 ions per second or greater)
Ions pass through channels down their
electrochemical gradient, which is a function of
ion concentration and membrane potential,
"downhill",without the input (or help) of metabolic
energy (e.g. ATP, co-transport mechanisms,
or active transport mechanisms)
18. HOW DO DRUGS WORK BY BLOCKING ION CHANNELS?
KEY CONCEPTS:
• Ion channels allow ions to transverse the cell membrane
through a pore and down an electrochemical gradient.
• Some drugs bind to ion channels and physically
block the pore or cause an allosteric change
that closes the pore.
• Changes in the intracellular concentration of ions mediates
the effects of inhibitors of ion channels.
19.
20. BIMM118
CALCIUM CHANNELS
• Extracellular compartment: (predominantly in nerve, cardiac and
smooth muscle cells)
Three types of plasma-membrane localized calcium channels:
– Voltage operated calcium channels:
Action potental depolarizes plasma membrane, which results in the
opening of “voltage” dependent calcium channels (channels can
be opened by increase in extracellular K+).
Each channel protein has four homologous domains, each
containing six membrane spanning -helices (the fourth one
functions as the “voltage” sensor.
21. BIMM118
CALCIUM CHANNELS
– Ligand gated calcium channels:
Calcium channels opened after ligand binding to the receptor (e.g.
glutamate/NMDA receptor; ATP receptor; nicotinic ACh receptors (
muscarinic ACh receptors signal through G-Proteins
--> slower), prostaglandin receptors
– Store operated calcium channels:
Activated by emptying of intracellular stores, exact mechanism
unknown
Type Properties Location/Function Blockers
L
High activation threshold;
slow inactivation
Plasma membrane of many cells; main
Ca++ source for contraction in smooth and
cardiac muscle
Dihydropyridines;
verapamil; diltiazem
N
Low activation threshold;
slow inactivation
Main Ca++ source for transmitter release
by nerve terminals
w-Conotoxin
(snail venom)
T
Low activation threshold;
fast inactivation
Widely distributed; important in cardiac
pacemaker and Purkinje cells
Mibefradil; (verapamil;
diltiazem)
Three types:
52. Encoded by 9 genes- CLCN1- CLCN9
Myotonia congenita (MC) was the first human disease
proven to be caused by an ion channel defect, thus
leading to the discovery of the CLCN1 gene encoding
the ClC-1 channel responsible for the high Cl
conductance of skeletal muscle membrane
Blockers – under development
Openers – Lubiprostone, approved by US FDA for
chronic constipation
CLC openers- useful for hereditary channelopathies &
epilepsies
In vitro study – ACTZ, intracellular biochemical
pathways
53. The -aminobutyric acid and glycine receptors
(GABA-A and GlyR) are the major inhibitory
neurotransmitter-gated receptors in the CNS
After neurotransmitter binding, the ingress of Cl ions
within the cell hyperpolarizes the postsynaptic
membrane, resulting in neurotransmission inhibition
No therapeutic ligands –- GlyR
BZDs & Phenobarbital – Epilepsies
Drugs acting on B3 subunit of GABA-A receptor -
Chronic Insomnia
Alpha1 & Gamma 2 mutations (GABA-A receptor) -
BZDs
54. Nicotinic ACh receptors, glutamate receptors,
and serotoninergic receptors
No effective NAch receptor modulator till now
in epilepsy & channelopathies
Glutamate antagonists – AD, PD, HC, ALS,
melanoma, neutopathic pain
HT3 receptor channel – antinociception &
antiemetics
Glutamate agonists – Schizophrenia (proposed)