Berbanes: A New Class of Selective α2-adrenoceptor Antagonists

E. Sylvester Vizi, Istvan Toth, George T. Somogyi, Lajos Szabo, Laszlo G. Harsing, Csaba Szantay

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Abstract

The a-adrenoceptor blocking properties of some berbanes have been studied and compared with those of idazoxan, yohimbine, phentolamine, and prazosin. Their effects on presynaptic α2-adrenoceptors were studied on chemical neurotransmission of isolated rat vas deferens and longitudinal muscle strip of guinea pig ileum; xylazine or norepinephrine was employed as agonist. The aradrenoceptor blocking activities of the berbanes were tested on isolated rat vas deferens and rabbit pulmonary artery by using phenylephrine or norepinephrine as agonist. The antagonistic activity of the berbanes and the reference compounds on a2- and α1-adrenoceptors was characterized by the apparent pA2values. of the compounds studied, [8aS*-(8aα,12aα,13aα:)]-llQ:-hydroxy-5,6,8a,9,10,ll,12,12a,13,13a-decahydro-8H-benzo[g]-l,3-benzodioxolo[5,6-a]quinolizine, 6d, proved to be the most selective antagonist at the presynaptic a2-adrenoceptors (a1:a2ratio = 1659). Since blockade of α2-adrenoceptors located on noradrenergic axon terminals leads to an increase of norepinephrine release, this compound could have potential as an antidepressant agent.

Original languageEnglish
Pages (from-to)1355-1359
Number of pages5
JournalJournal of Medicinal Chemistry
Volume30
Issue number8
DOIs
Publication statusPublished - Aug 1 1987

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ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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