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![Example of G-Protein Coupled receptor
Sr no. Receptors Types
1 Muscarinic receptors [M1-M5]
2 Adrenergic receptors [α and β]
3 Histamine receptors [H1-H3]
4 Dopamine receptors [D1-D5]
5 Opiod receptors [μ κ б]
6 5-HT receptors 5-HT[1-7] except 5-
HT3
7 GABAB receptors GABAB](https://image.slidesharecdn.com/receptors-converted-230118144634-46b9da34/75/Receptors-12-2048.jpg)
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Receptors
- 1. Prepared by-Shagufta Farooqui AssistantProfessor Department of Pharmacology Nanded Pharmacy college,Nanded
- 2. Receptors These are themolecules or binding site located on the surface or inside the cell that recognise the signal molecule or drug and indicate the response. Chemically receptors are protein in nature .All the receptors are proteins but all the proteins are not receptors.
- 3. Types of Receptors G-Protein Coupled receptor Ligand gatedion channel receptor Enzymatic receptors Nuclear receptors
- 4.
- 5. The G protein-coupledreceptor (GPCR) superfamily comprises the largest and most diverse group of proteins in mammals. Synonym: “seven-transmembrane” (7-TM), “serpentine” receptors, heptahelical receptors, serpentine receptor, and G protein–linked receptors (GPLR)
- 6. It is involvedin information transfer (signal transduction) from outside the cell to the cellular interior. 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. ~45% of all pharmaceutical drugs are known to target GPCRs.
- 7. Adenyl cyclase pathway ATPCAMP Inactive Adenyl cyclase Phodphodiesterase Secondary Messenger
- 8. CAMP Effects onorgan- Cardiac muscle Increases force of contraction, Increase Heart rate, Increases Blood pressure. Smooth muscle Smooth relaxation Adipose tissue Lipolysis Liver Glycogenolysis
- 9. Phopholipase pathway Stimulation ofthis pathway results in the breakdown of cell membrane phospholipids. Phospholipids upon breakdown will release ionsitol-1,4,5 –triphosphate (IP3) and diaceylglycerol (DAG) which acts as a secondary messenger.
- 10. Sr no. OrganPharmacological action 1 Increases force of contraction, Increase Heart rate, Increases Blood pressure. 2 Smooth muscle contraction 3 Increase secretion 4 CNS stimulation
- 11. All G-protein couplereceptors mediate pharmacological action through release of second messenger ,but the type of second messenger is different from one receptor to another receptor. The type of second messenger will be identified by following representation. G-protein Signalling pathway Gs Increase CAMP Gi Decrease CAMP Gq Increase IP3,DAG
- 12. Example of G-ProteinCoupled receptor Sr no. Receptors Types 1 Muscarinic receptors [M1-M5] 2 Adrenergic receptors [α and β] 3 Histamine receptors [H1-H3] 4 Dopamine receptors [D1-D5] 5 Opiod receptors [μ κ б] 6 5-HT receptors 5-HT[1-7] except 5- HT3 7 GABAB receptors GABAB
- 13.
- 15. Receptors Organs Responseeffects M1 Gastric Parietal cells(oxyntic cells) 2.Cilliary muscles of iris Contraction of Parietal cells, Contraction of muscle increase acid secretion Decrease pupil size M3 Smooth muscle a) Bronchi b) Uterus c) GIT 2.Glands a) Sweat gland b) Salivary gland c) Lacrimal glands a)constriction of bronchi b) constriction of uterus c) constriction of GIT a) Increase secretion b) Increase salivary secretion c) Lacrimal secretion c) Increase peristalsis M5 CNS Stimulation
- 16. Receptors organs Response M2(Gi)Heart Decrease heart rate, Decreases force of contraction, Decrease cardiac output, Decrease heart rate M4(Gi) CNS Inhibitory effect on CNS
- 17. Acetylcholine is aneurotransmitter in parasympathetic nervous system and this is also known as cholinergic nervous system. Drugs which produces action similar to acetylcholine called as parasympathetic or cholinomimetics or cholinergic drugs or agonist. Drugs which block the action of acetylcholine called as parasympatholytics/ Anti cholinergic drugs/cholinergic receptor blockers. Uses of Anticholinergic drugs: Anti hypotensive Bronchodilators Anti diarrheal Anti-ulcer
- 18. Anti hypertensive Constipation Achlorhydria Uses ofCholinergic drugs:
- 19.
- 20. Adrenergic Receptors Sr no.Receptor Function 01 Beta1-Heart Increase Force of contraction , Increase blood pressure, Increase heart rate 02 Beta2-Smooth muscle Liver Bronchi Relaxation Glycogenolysis Bronchodilation 03 Beta3- Adipose tissue Lipolysis
- 21. Uses of Adrenergicdrugs Anti hypotensive Bronchodilators Antihistamine
- 22. Ionotropic Receptors These receptorsare also transcellular receptors. Here the receptors are coupled to ion channel. When the ligand binds to the receptors ,There will be opening of ion channels will takes place that results in either influx or efflux of ion depending upon concentration gradient and which will produce pharmacological action. Example of Ionotropic receptors. Sr no. Examples of receptors 1 Nicotinic receptors 2 5-HT3 receptors 3 GABAA receptors 4. NMDA receptors
- 23. 1. Nicotinic receptors Acetylcholine Nm(Skeletalmuscles) Na+ Skeletal muscles Contraction
- 24.
- 25. 3. GABAA receptors GABA GABAA(CNS) CL- CNS Depression
- 26. 4.NMDA receptors Aspartate andglutamate NMDA(CNS) Ca++ CNS Stimulation
- 27. Enzymatic Receptors These receptorsare coupled to enzymes. There are also transcellular receptors. When the ligand binds to receptors, enzymes automatically undergoes phosphorylation (Autophosphorylation) which is responsible for mediating pharmacological action. Most of the receptors coupled to the enzymes tyrosine kinase. E.g- 1. Insulin receptors-Tyrosine kinase 2. Growth factor receptors-Tyrosine kinase 3. Natriuretic peptide receptors- Guanyl cyclase
- 28. Nuclear Receptors Here receptorsare coupled to nucleus .These receptors are Intracellular . When ligand binds to receptors Direct change in the gene Expression (DNA) Synthesis of specific m- RNA Synthesis of specific protein Produces Pharmacological Action
- 30. Most of thesteroidal drugs and steroidal hormones produces their actions through nuclear receptors. Hence they are also called as steroidal receptors. Example- 1. Glucocorticoid receptors. 2. Mineral corticoid receptors 3. Estrogen receptors 4. Progesterone receptors 5. Testosterone receptors 6. Viamine A and Vitamin D 7. Thyroid hormone receptors.