Antiaggregatory activity

A phenyl ethanol amine in which the nitrogen is alkylated by a long chain alphatic group departs in activity from the prototypes. This agent, suloctidil (43) is described as a peripheral vasodilator endowed with platelet antiaggregatory activity. As with the more classical compounds, preparation proceeds through bromination of the substituted propiophen-one ( ) and displacement of halogen with octyl amine. Reduction, in this case by means of sodium borohydride affords suloctidil (43). ... 

Compared with other NO-releasers like nitrates, Molsidomine and other sydnonimines like Pirsidomine 87 [117] and C89-4095 89 [118] show diminished or no development of tolerance and a higher antiaggregatory activity in platelets [119]. 

Park, S. Wanna, L. Johnson, M. E. Venton, D. L. 2000. A mass spectrometry screening method for antiaggregatory activity of proteins covalently modified by combinatorial library members application to sickle hemoglobin. /. Comb. Chem., 2,314-317. 

Yin K, Hahishka PV, Yan Y-T, Wong PY-K. Antiaggregatory activity of 8-epi-prostaglandin Fj, and other F-series prostanoids and their binding to thromboxane Aj/ prostaglandin receptors in human platelets. J Pharmacol Exp Ther 1994 270 1192-6... 

Nanimiya S, Okuma M, Ushikubi F. Binding of aradioicxlinated 13-azapinane thromboxane antagonist to platelets correlation with antiaggregatory activity in different spedes. Br J Pharmacol 1986 88 323-31... 

Compd. Binding assay (Ki, nM)e Adenylate cyclase (ECsn, nM)e Functional activity (ECso, nM) Antiaggregatory activity (ICso, nM) ... 

Moreover, Dionisotti and coworkers evaluated in vivo rabbit platelet accumulation in response to ADP, given either before or after drug infusion. NECA, and, to higher extent, HENECA clearly decreased platelet accumulation in the rabbit. This antiaggregatory activity is of short duration, and does not appear to be due to hemodynamic changes, but rather is a result of selective drug action on platelet adenosine receptors [25]. In the same experiment the selective Ai adenosine agonist CCPA resulted inactive. 

Antiaggregatory activity (potency ratio vs NECA)<= Rabbit platelets... 

Siluk D, Kaliszan R, Haber P, Petrusewicz J, Brzozowski Z, Sut G. Antiaggregatory activity of hypoglycaemic sulphonylureas. Diabetologia 2002 45(7) 1034-1037. 

Narumiya, S., Okuma, M. and Ushikubi, F. (1986). Binding of a radioiodinated 13-azapinane thromboxane antagonists to platelets Correlation with antiaggregatory activity in different species. Br. ]. Pharmacol, 88, 323-331... 

Panayiotou, A. Samartzis, D. Nomikos, T. Fragopoulou, E. Karantonis, H.C. Demopoulos, C.A. Zabetakis, I. (2000). Lipid fractions with aggregatory and antiaggregatory activity toward platelets in fresh and fried cod (Gadus morhua) correlation with platelet-activating factor and atherogenesis. Journal of Agricultural and Food Chemistry, Vol.48, No.l2, Pecember 2000), pp. 6372-6379, ISSN 0021-8561. 

Monge A., Aldana I., Losa M.J., and etc. Newpyridazino[4,5-b]indole derivatives with inodilator and antiaggregatory activities - Arzneim-Forsch., 1993,v.43,p. 1175-80. 

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