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

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

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Department of Chemistry, Synaptic Pharmaceutical Corporation, Paramus, NJ 07652, USA.


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.

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