PMID: 8955864Nov 1, 1996Paper

Pharmacological evaluation of prazosin- and doxazosin-related compounds with modified piperazine ring

Arzneimittel-Forschung
Dario GiardinàM Massi

Abstract

New doxazosin-related compound (1-3) with a N,N'-dimethyl alkanediamine chain replacing the piperazine ring, have been synthesized and their pharmacological properties have been tested together with some prazosin analogues (4-8) bearing either a similar structural modification or a substituted piperazine moiety. In the in vitro study, on alpha 1- and alpha 2-adrenoceptors of rat vas deferens tissues, 1-3 displayed high alpha 1-antagonist activity, 2 and 3 being equipotent to doxazosin but markedly less selective in respect to alpha 2-adrenoceptors. Replacement of the piperazine ring with an alkanediamine chain resulted in a strong fall in alpha 1-selectivity, owing to increased alpha 2-antagonist activity, as in the prazosin-related series. In in vivo studies, the antihypertensive activity of tested compounds was investigated on spontaneously hypertensive rats (SHR) following both intragastric (IG) and intraperitoneal (OP) administration. Among the tested compounds, 7 and 8, which conserved a substituted piperazine ring, proved the most interesting drugs displaying a marked hypotensive effect. The other prazosin- and doxazosin-related compounds, in which an alkanediamine chain replaced the piperazine nucleus, showed an antihype...Continue Reading

Related Concepts

Related Feeds

Antihypertensive Agents: Mechanisms of Action

Antihypertensive drugs are used to treat hypertension (high blood pressure) which aims to prevent the complications of high blood pressure, such as stroke and myocardial infarction. Discover the latest research on antihypertensive drugs and their mechanism of action here.

Adrenergic Receptors: Trafficking

Adrenergic receptor trafficking is an active physiological process where adrenergic receptors are relocated from one region of the cell to another or from one type of cell to another. Discover the latest research on adrenergic receptor trafficking here.