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11 Cards in this Set
- Front
- Back
Bmax
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also = R(0)
the maximal number of receptors available--> because a set amount, receptors are saturable |
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K(D)
|
affinity of a hormone to a receptor--> measured in units of hormone concentration
lower K(D) = higher affinity higher K(D) = lower affinity |
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EC50
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the hormone concentration that gives 1/2 of the cellular response
generally EC50 < K(D) |
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Scatchard plot
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X-intercept = Bmax
K(D) = -1/slope -->the higher the absolute value of the slope, the higher the affinity of the hormone for the recptor |
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Membrane-bound vs. Intracellular Receptors
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Membrane-bound = peptide and proteins
Intracellular = thyroid and steroid |
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Gαs
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β-adrenergic amines, glucagon, parathyroid hormone, many others
--> stimulate adenylate cyclase |
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Gαi
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Acetylcholine, α-adrenergic amines, many neurotransmitters
-->inhibits adenylate cyclase |
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Gαt
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Photons
-->stimulates cGMP phosphodiesterase |
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Gαq
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Acetylcholine, α-adrenergic amines, many neurotransmitters
-->increases IP3 and intracellular calcium |
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Gα13
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Thrombin, orther agonists
-->stimulates Na+ and H+ exchange |
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Gαq transduction pathway
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Gαq --> stimulates phospholipase C-β (PLC)
PLC --->cleaves PIP2 ---> produce IP3 and DAG IP3 --> increase Ca2+ release from ER DAG + Ca2+ --> stimulates PKC -->phosphorylates substrates to regulate growth and secretion |