Diethyl 3,6-dihydro-2,4-dimethyl-2,6-methano-1,3-benzothiazocine-5,11- dicarboxylates as calcium entry antagonists: new conformationally restrained analogues of Hantzsch 1,4-dihydropyridines related to nitrendipine as probes for receptor-site conformation.

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Baldwin JJ, Claremon DA, Lumma PK, McClure DE, Rosenthal SA, Winquist RJ, Faison EP, Kaczorowski GJ, Trumble MJ, Smith GM

Diethyl 3,6-dihydro-2,4-dimethyl-2,6-methano-1,3-benzothiazocine-5,11- dicarboxylates as calcium entry antagonists: new conformationally restrained analogues of Hantzsch 1,4-dihydropyridines related to nitrendipine as probes for receptor-site conformation.

J Med Chem. 1987 Apr;30(4):690-5.

PubMed ID

2435904 [ View in PubMed

]

Abstract

The pharmacological activity of rigid analogues of 1,4-dihydropyridine calcium entry antagonists 9-16 is demonstrated by dose-dependent inhibition of the calcium contraction in depolarized rat aortic strips and by a [3H]nitrendipine binding assay in using cardiac sarcolemmal membranes. From the results, a model is proposed as the receptor-bound conformation of the dihydropyridine calcium entry antagonists.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Nifedipine	Voltage-dependent L-type calcium channel subunit alpha-1C	Ki (nM)	1	N/A	N/A	Details
Nitrendipine	Voltage-dependent L-type calcium channel subunit alpha-1C	Ki (nM)	0.25	N/A	N/A	Details