Intracellular calcium release in N1E-115 neuroblastoma cells is mediated by the M1 muscarinic receptor subtype and is antagonized by McN-A-343.
Experiments using muscarinic receptor antagonists were done to determine which muscarinic receptor subtypes(s) mediate carbachol-evoked calcium release in N1E-115 cells. McN-A-343 and a new analog, (+/-)BN228, were weak antagonists and neither compound caused release on its own. The rank order of potency was 4-DAMP greater than pirenzepine greater than AFDX116 greater than (+/-)BN228 and McN-A-343. This profile, pirenzepine's high potency (19-fold greater than AFDX116) and its IC50 of 31 nM suggest that calcium release in this neuronal cell line is mediated by the M1 muscarinic receptor subtype.
Mathes
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C
Hopkins Marine Station, Stanford University, Pacific Grove, CA 93950.
Wang
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SS
Vargas
H M
HM
Thompson
S H
SH
D008455:(4-(m-Chlorophenylcarbamoyloxy)-2-butynyl)trimethylammonium Chloride / Q000494:pharmacology*; D000818:Animals; D002118:Calcium / Q000378:metabolism*; D002121:Calcium Channel Blockers / Q000494:pharmacology*; D002217:Carbachol / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D007425:Intracellular Membranes / Q000378:metabolism*; D018727:Muscarinic Antagonists; D009447:Neuroblastoma / Q000378:metabolism* / Q000473:pathology; D010277:Parasympathomimetics / Q000494:pharmacology; D011976:Receptors, Muscarinic / Q000502:physiology*; D014407:Tumor Cells, Cultured
D002121:Calcium Channel Blockers; D018727:Muscarinic Antagonists; D010277:Parasympathomimetics; D011976:Receptors, Muscarinic; D008455:(4-(m-Chlorophenylcarbamoyloxy)-2-butynyl)trimethylammonium Chloride; D002217:Carbachol; D002118:Calcium