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Adrenergic receptors

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Adrenoceptors are membrane 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.

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Adrenergic receptors

  1. 1. 1
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  3. 3. INTRODUCTI ON  Adrenoceptors are membrane 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
  4. 4. CLASSIFICATI ON 4
  5. 5. 5 RECEPTORNAME TYPICALLOCATIONS α1 Vascular smooth 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. 6. 1. α ADRENERGIC RECEPTOR 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
  7. 7. AGONISTS Phenylephrine Xylometazoline Pseudoephedrin e Naphazoline ANTAGONISTS Prazosin Terazosin Alfuzosin Doxazosin 7
  8. 8. 8
  9. 9. B) α2 ADRENERGIC RECEPTOR (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
  10. 10. AGONIST Clonidine Methyl dopa Guanabenz Guanfacine ANTAGONIST Yohimbine Mirtazapine Idazoxan Atipamezole 10
  11. 11. 11
  12. 12. 12
  13. 13. 2. β ADRENERGIC RECEPTORS A) β1 ADRENERGIC RECEPTOR (Gs) 13
  14. 14. AGONIST • Denopamine • Dobutamine • Xamoterol ANTAGONIST • Atenolol • Metoprolol • Esmolol • Nebivolol • Bisoprolol 14
  15. 15. B) β2 ADRENERGIC RECEPTORS- 15
  16. 16. • Salbutamol • Levosalbutamol • Terbutaline AGONIST • Butoxamine ANTAGONIST 16
  17. 17. C) β3 ADRENERGIC RECEPTORS- 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
  18. 18. 18
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  20. 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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Adrenoceptors are membrane 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.

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