Competitive inhibition of phosphoinositide hydrolysis by the muscarinic receptor antagonist AF-DX 116 is of low affinity in mouse cerebral cortex期刊界 All Journals 搜尽天下杂志传播学术成果专业期刊搜索期刊信息化学术搜索

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Competitive inhibition of phosphoinositide hydrolysis by the muscarinic receptor antagonist AF-DX 116 is of low affinity in mouse cerebral cortex

Authors:	Thomas L Smith and Henry I Yamamura

Institution:	^aVeterans Administration Medical Center, Tucson, AZ 85723 U.S.A. ^bDepartment of Pharmacology, University of Arizona Health Sciences Center, Tucson, AZ 85724 U.S.A.

Abstract:	Carbamylcholine stimulated ³H]inositol phosphate accumulation in mouse cerebral cortical slices with an ED₅₀ value of approximately 70 μM. Increasing concentrations of the M₂ selective muscarinic cholinergic receptor antagonist, AF-DX 116 (0.3–3.0 μM), produced parallel shifts to the right for concentration-response curves to carbamylcholine. A pA₂ value for AF-DX 116 of 6.5 (low affinity) was obtained frommSchild plot analysis. It is concluded that the M₂ muscarinic receptor subtype, as defined by high affinity ³H]AF-DX 116 radioligand binding, is not appreciably coupled to polyphosphoinositide hydrolysis in the mouse cerebral cortex.

Keywords:	Cerebral cortex Muscarinic cholinergic receptor Carbamylcholine Inositol phosphate Pirenzepine AF-DX 116
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