Muscarinic acetylcholine receptor

作者: E HEILBRONN , T BARTFAI

DOI: 10.1016/0301-0082(78)90011-4

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摘要: ABSTRACT Muscarinic acetylcholine receptors from rat cerebral cortex and small intestine were studied by the high affinity specific activity antagonists 3 H-3-quinuclidinyl benzilate (3-QNB) (29.4 Ci/mmol) H-N-methyl-4-piperidinyl (4-NMPB) (55.4 Ci/mmol). Equilibrium binding data combined with studies on association dissociation rates of receptor antagonist complex are compatible reaction sequence: A + R ⇆ AR * where stand for antagonist, respectively. For both class equilibrium constant isomerization step was 0.15 in phosphate buffer (Jarv co-workers, 1979). The results agonist carried out under conditions can be described as if there two classes sites affinities 100 μM 0.05 carbamylcholine (Hedlund Bartfai, It appears that it is low site associated muscarinic activation cyclic GMP synthesis cortical slices N1E 115 neuroblastoma cells. In latter controls a non-voltage dependent Ca 2+ channel (Study 1978) . Calcium blocking agents such D600 Co inhibit mediated rise levels. Experiments cardiotoxin V II 2 N. m. mossambica (supplied Dr. L. Visser) indicate may share some common receptor-coupled channel, or itself.

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