57005-09-1Relevant academic research and scientific papers
New non peptidic C5a receptor antagonists
Astles, Peter C.,Brown, Thomas J.,Cox, Paul,Halley, Frank,Lockey, Peter M.,McCarthy, Clive,McLay, Iain M.,Majid, Tahir N.,Morley, Andrew D.,Porter, Barry,Ratcliffe, Andrew J.,Walsh, Roger J.A.
, p. 907 - 912 (2007/10/03)
A series of phenylguanidines which bind to the C5a receptor has been developed. The lead compound 1 (IC50 = 30 μM), discovered through random screening, has been modified to provide 32 (RPR121154) with submicromolar activity. This compound was
Cardiovascular activity of aromatic guanidine compounds.
Hughes et al.
, p. 1077,1080 (2007/10/04)
A series of aromatic guanidines and several 1-phenylbiguanides was prepared and tested for cardiovascular (CV) effects in anesthetized dogs measuring heart rate, blood pressure, carotid artery blood flow, and myocardial force changes. The predominant CV effect at minimally effective dose was vasoconstriction unassociated with cardiac stimulation. The structure-activity relationships of the compounds were discussed comparing their structural similarities to the beta-phenylethylamines. The most potent members of the series were phenylguanidines substituted in the 3 and 4 positions on the aromatic nucleus with hydroxy or chloro groups. Preliminary mechanism studies indicated that the 3,4-dihydroxyphenylguanidines act at least partially by a direct alpha-adrenergic mechanism
