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In vitro and in vivo studies on the effects of the alpha‐adrenoceptor blocker IP/66 (1‐(2‐ethoxy‐2‐(3′ ‐pyridyl)ethyl)‐4‐(2′‐methoxy‐phenyl)piperazine) on urethral tone in rats
Author(s) -
Manzini Stefano,
Perretti Francesca,
Boni Paola,
Barbanti Gabriele,
Turini Damiano,
Maggi Carlo Alberto
Publication year - 1991
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/ddr.430230104
Subject(s) - phenylephrine , prazosin , in vivo , pharmacology , chemistry , piperazine , alpha (finance) , adrenergic receptor , endocrinology , medicine , antagonist , biology , receptor , blood pressure , biochemistry , construct validity , microbiology and biotechnology , nursing , patient satisfaction
IP/66 (1‐(2‐ethoxy‐2‐(3′‐pyridyl)ethyl)‐4‐(2′‐methoxy‐phenyl))piperazine is a newly synthetized and stereoselective alpha‐adrenoceptor blocking drug. This compound exhibits preferential blocking activity in postjunctional as compared to prejunctional alpha‐adrenergic responses. Furthermore, IP/66 inhibits phenylephrine‐induced motor response in human and rat prostatic tissue and phenylephrine‐, DMPP‐ and EFS‐induced motor responses in rat urethral tissues, being equieffective or even more potent than prazosin. Like prazosin, intravenous administration of IP/66, at doses at which no hypotensive effect is observed, induces a marked inhibition of phenylephrine or DMPP‐induced increase in urethral perfusion pressure, in anaesthetized pithed rats. Finally, IP/66 administration exerts beneficial effects in animals with surgically‐ or pharmacologically‐induced urethral outflow obstruction. As a whole, the pharmacodynamic profile of IP/66 is promising and this drug might be proposed for clinical setting evaluating its efficacy for the treatment of lower urinary tract dysfunctions.