Alpha 1b adrenergic receptor antagonists

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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514255, 514260, 544116, 544291, A61K 31535, A01N 4360, C07D41500, C07D23972

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active

057474907

ABSTRACT:
This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha 1b adrenergic receptor antagonists. These compounds display submicromolar affinity for the human alpha 1b adrenergic receptor subtype while displaying at least five-fold lower affinity for the human alpha 1d and alpha 1a adrenergic receptor subtypes, and many other G-protein coupled human receptors. One application of these compounds is in the treatment of hypertension. More specifically, these compounds display selectivity for lowering blood pressure without, for example, substantially affecting urethral pressure.

REFERENCES:
patent: 3517005 (1970-06-01), Cronin et al.
patent: 4287341 (1981-09-01), Hess et al.
patent: 4352928 (1982-10-01), Hiranuma et al.
patent: 4749705 (1988-06-01), Tomiyama et al.
patent: 5064833 (1991-11-01), Ife et al.
Phife et al., Bioorganic & Medicinal Chemistry Letters, "Marine Sponge Bis(Indole) Alkaloids That Displace Ligand Binding to a1 Adrenergic Receptors" vol. 6, No. 17, pp. 2103-2106, 1996.
Giardina et al., J. Med. Chem., "Synthesis and Biological Profile of the vol. 39, pp. 4602-4607, (1996).
Giardina et al., European Journal of Pharmacology, "Receptor binding profile of cyclazosin, a new a1B-adrenoceptor antagonist", vol. 287, pp. 13-16, (1995).

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