146929-33-1Relevant articles and documents
USE OF SELECTIVE ANTAGONISTS OF THE ALPHA 1b-ADRENERGIC RECEPTOR FOR IMPROVEMENT OF SEXUAL DYSFUNCTION
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Page/Page column 11, (2010/02/14)
Described is the use in the treatment of either male or female sexual dysfunction of selective antagonists of the alpha1B-adrenergic receptor and the pharmaceutical compositions containing them as compounds capable of helping the sexual act avoiding at th
Structure-Activity Relationships in Prazosin-Related Compounds. 2. Role of the Piperazine Ring on α-Blocking Activity
Giardina, Dario,Gulini, Ugo,Massi, Maurizio,Piloni, Maria G.,Pompei, Pierluigi,et al.
, p. 690 - 698 (2007/10/02)
Several prazosin-related compounds have been synthesized and evaluated for their blocking activity toward α-adrenoreceptors.The structural modification performed on the prazosin structure included the replacement of the piperazine ring with 2,3-dialkylpiperazine or 1,2-cyclohexanediamine moieties to characterize a lipophilic binding pocket in the α1 adrenoreceptor surface.Cyclohexanediamine derivatives 3-6 were almost devoid of potency and selectivity, whereas dialkylpiperazine compounds 7-14 showed high affinity and selectivity toward α1-adrenoreceptors.The cis derivative 13 (cyclazosin) was the most potent and selective with an α1/α2 selectivity ratio value of 7800.The particular trend of antagonist activity within cis/trans stereoisomeric compounds not only supports the presence of a lipophilic binding area on α1-adrenoreceptor surface but also suggests that the lipophilic pocket is endowed with a well-defined size and spatial orientation.The most active compound of the series, 13, was tested also in vivo for antihypertensive activity on spontaneously hypertensive rats.It showed an interesting long-lasting hypotensive effect, very similar to that of doxazosin, which was statistically significant 12 h after oral administration.