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General pharm
G-protein linked second messengers
Term | Definition |
---|---|
alpha-1 receptor | Gq increase vascular s. muscle contraction, increase pupillary dilator m. contraction (mydriasis), increase intestinal and bladder sphincter m. contraction |
alpha 2 receptor | Gi decrease sympathetic outflow, decrease insulin release, decrease lipolysis, increase platelet aggregation, decrease aqueous humor production |
Beta 1 receptor | increase HR, contractility, renin release, lipolysis Gs |
Beta 2 receptor | Gs Vasodilation, bronchodilation, increase lipolysis, increase insulin release, decrease uterine tone , ciliary m relaxation, increase aqueous humor prod. |
Beta 3 receptor | Gs increase lipolysis, increase thermogenesis in s. muscle |
M1 receptor | Gq CNS, enteric nervous system |
M2 receptor | Gi decrease HR and contractility of the atria |
M3 receptor | Gq increase exocrine gland secretions, increase gut peristalsis, increase bladder contraction, bronchoconstriction, increase pupillary sphincter m. contraction (miosis), ciliary m contraction (accommodiation) |
D1 receptor | Gs relaxes renal vascular s. muscle, activates direct pathway of striatum |
D2 receptor | Gi Modulates transmitter release in the brain, inhibits indirect pathway of striatum |
H1 receptor | Gq increase nasal adn bronchial mucus prod., increase vascular permeability, contraction of bronchioles, pruritus, pain |
H2 receptor | Gs increase gastric acid secretion |
V1 receptor | Gq increase vascular smooth m. contraction |
V2 receptor | Gs increase H2O permeability and reabsorption in collecting tubules of kidney |
Gq | Activation of phospholipase C In lipids, phospholipase C breaks PIP2--> DAG and IP3 DAG--->Protein Kinase C IP3--> increase intracellular Ca2+ concentration---> smooth m. contraction |
Gs | activation of adenylate cyclase--> ATP converted to cAMP cAMP activates protein kinase A--->increase intracellular Ca2+ concentration in heart |
Gi | Inhibits adenylate cyclase decrease cAMP--->no cAMP dependent protein kinase ---> inhibition myosin light chain kinase (smooth m.) |