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Adrenergic receptors
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- 3. INTRODUCTI ON Adrenoceptors aremembrane bound receptors located throughout the body on neuronal and non- neuronal tissues where they mediate a diverse range of responses to the endogenous catecholamines- noradrenaline and adrenaline. They are G protein coupled receptors. Binding of catecholamine to the receptor is responsible for fight or flight response. 3
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- 5. 5 RECEPTORNAME TYPICALLOCATIONS α1 Vascularsmooth muscle, visceral smooth muscle, radial smooth muscle of iris, CNS neurons α2 Some presynaptic terminals, pancreatic islets, platelets, ciliary epithelium, smooth muscles, CNS neurons β1 Myocardium, JG cells, some presynaptic terminals, CNS neurons β2 Visceral smooth muscle, vascular smooth muscle, liver, myocardium, skeletal muscle, some presynaptic terminals, CNS neurons
- 6. 1. α ADRENERGICRECEPTOR A) α1 ADRENERGIC RECEPTOR (Gq) ACTIVATION Gq activates phospholipas e C Increase in Inositol phosphate 3 (IP3) and Calcium Activation of enzyme protein kinase C Phospho rylation of other enzymes Increase or decrease of electrolyte transfer in or out of the cell 6
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- 9. B) α2 ADRENERGICRECEPTOR (Gi) ACTIVATION Gi associates with adenylyl cyclase Decrease in cAMP Protein Kinase A (PKA) is not activated by cAMP Proteins such as phosphorylase kinase cannot be phosphorylated by PKA No activation of glycogen phosphorylase Decreased breakdown of glycogen 9
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- 13. 2. β ADRENERGICRECEPTORS A) β1 ADRENERGIC RECEPTOR (Gs) 13
- 14. AGONIST • Denopamine • Dobutamine •Xamoterol ANTAGONIST • Atenolol • Metoprolol • Esmolol • Nebivolol • Bisoprolol 14
- 15. B) β2 ADRENERGICRECEPTORS- 15
- 16. • Salbutamol • Levosalbutamol •Terbutaline AGONIST • Butoxamine ANTAGONIST 16
- 17. C) β3 ADRENERGICRECEPTORS- They are involved in the epinephrine and norepinephrine induced activation of adenylyl cyclase through the action of the G proteins of the type Gs. • Ambigeron • Mirabegron • Solabegron AGONIST • L-748,328 • L- 748,337 ANTAGONIST 17
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- 20. REFERENCES 20 Adrenoceptor Pharmacology,Emma Robinson and Alan Hudson, Psychopharmacology Unit, Department of Pharmacology, School of Medical Sciences, University of Bristol. www.cvpharmacology.com/vasodilator/alpha www.ncbi.nih.gov/pubmed/6098436 www.wikipedia.com
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