Design and synthesis of novel dihydropyridine alpha-1a antagonists.

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Marzabadi MR, Hong X, Nagarathnam D, Miao SW, Chiu G, Wong WC, Wetzel JM, Fang J, Forray C, Chen TB, O'Malley SS, Chang RS, Gluchowski C

Design and synthesis of novel dihydropyridine alpha-1a antagonists.

Bioorg Med Chem Lett. 1999 Oct 4;9(19):2843-8.

PubMed ID

10522703 [ View in PubMed

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Abstract

A series of analogs of SNAP 5150 containing heteroatoms at C2 or C6 positions is described. Herein, we report that the presence of alkyl substituted heteroatoms at the C2(6)-positions of the dihydropyridine are well tolerated. In addition, 15 inhibited the phenylephrine induced contraction of dog prostate tissue with a Kb of 1.5 nM and showed a Kb (DBP, dogs, microg/kg)/Kb (IUP, dogs, microg/kg) ratio of 14.8/2.5.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Prazosin	Alpha-1A adrenergic receptor	Ki (nM)	0.58	N/A	N/A	Details
Prazosin	Alpha-1B adrenergic receptor	Ki (nM)	0.55	N/A	N/A	Details
Prazosin	Alpha-1D adrenergic receptor	Ki (nM)	0.33	N/A	N/A	Details