TY - JOUR
T1 - Inhibition of cyclic AMP formation in N1E-115 neuroblastoma cells is mediated by a non-cardiac M2 muscarinic receptor subtype
AU - Surichamorn, Wanida
AU - Amrhein, Carla L.
AU - Forray, Carlos
AU - El-Fakahany, Esam E.
N1 - Copyright:
Copyright 2014 Elsevier B.V., All rights reserved.
PY - 1989/7/31
Y1 - 1989/7/31
N2 - The cardioselective muscarinic antagonist, AF-DX 116 ((11[2-[(diethyl-amino)-methyl]-O-1-piperidinyl]-5,11-dihydro-6H-pyrido-[2,3-b][1,4]-benzodiazepine-6-one), was weak at blocking the M2 muscarinic receptor-mediated inhibition of cyclic adenosine monophosphate (cAMP) formation in mouse neuroblastoma cells (clone N1E-115). In contrast, the glandular-selective antagonists, hexahydro-sila-difenidol (HHSiD) and 4-diphenylacetoxy-N-methyl-pipedinine methiodide (4-DAMP), were quite potent at inhbiting this response, being 14- and 318-fold more potent than AF-DX 116 in this regard, respectively. According to the rank order of potency of these two classes of antagonists, these data provide the first pharmacological evidence that inhibition of cAMP formation in a neuronal tissue is mediated by a non-cardiac M2 muscarinic receptor subtype.
AB - The cardioselective muscarinic antagonist, AF-DX 116 ((11[2-[(diethyl-amino)-methyl]-O-1-piperidinyl]-5,11-dihydro-6H-pyrido-[2,3-b][1,4]-benzodiazepine-6-one), was weak at blocking the M2 muscarinic receptor-mediated inhibition of cyclic adenosine monophosphate (cAMP) formation in mouse neuroblastoma cells (clone N1E-115). In contrast, the glandular-selective antagonists, hexahydro-sila-difenidol (HHSiD) and 4-diphenylacetoxy-N-methyl-pipedinine methiodide (4-DAMP), were quite potent at inhbiting this response, being 14- and 318-fold more potent than AF-DX 116 in this regard, respectively. According to the rank order of potency of these two classes of antagonists, these data provide the first pharmacological evidence that inhibition of cAMP formation in a neuronal tissue is mediated by a non-cardiac M2 muscarinic receptor subtype.
KW - 4-Diphenlacetoxy-n-methyl-piperidine methiodide
KW - AF-DX 116
KW - Hexahydro-sila-difenidol, Cyclic adenosine monophosphate
KW - Muscarinic receptor subtypes
KW - N1E-115 neuroblastoma
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UR - http://www.scopus.com/inward/citedby.url?scp=0024412373&partnerID=8YFLogxK
U2 - 10.1016/0006-8993(89)91166-9
DO - 10.1016/0006-8993(89)91166-9
M3 - Article
C2 - 2548669
AN - SCOPUS:0024412373
SN - 0006-8993
VL - 493
SP - 320
EP - 325
JO - Brain Research
JF - Brain Research
IS - 2
ER -