Relationships between chemical structure and inhibition of epinephrine-induced human blood platelet aggregation.
The effect of structural features in a series of carbamoylpiperidine and nipecotoylpiperazine congeners on epinephrine-induced aggregation of human blood platelets is examined. Epinephrine-induced primary aggregation is effectively inhibited by the nipecotoylpiperazine derivatives (culminating at an IPA50 of 11.9 microM). While among nipecotoylpiperazine as well as carbamoylpiperidine congeners there are potent inhibitors of ADP-stimulated platelet function (cresting at an IA50 of 12.4 and 11.4 microM, respectively), the carbamoylpiperidine analogs are much less active (e.g., IPA50 of 298.1), or practically inactive, in impeding epinephrine-induced primary aggregation (PA).
Department of Medicinal Chemistry, College of Pharmacy, University of Tennessee, Memphis 38163.
J
J
Petrusewicz
A
A
Lasslo
G
G
Carter-Burks
R
R
Gollamudi
E O
EO
Dillingham
S E
SE
Bond
D000244:Adenosine Diphosphate; D004837:Epinephrine; D006801:Humans; D010880:Piperidines / Q000494:pharmacology*; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D015016:Yohimbine / Q000494:pharmacology
D010880:Piperidines; D010975:Platelet Aggregation Inhibitors; D015016:Yohimbine; D000244:Adenosine Diphosphate; D004837:Epinephrine