Abstract:
:The object of this study was to investigate the binding affinity of a newly synthesized 5-HT2 antagonist, (N-[2-[4-(5H-dibenzo[a,d]cyclohepten-5-ylidene)-piperidino]ethyl]-1-formyl-4-piperidinecarboxamide monohydrochloride monohydrate) (AT-1015), in the rabbit platelet membrane using [3H]-ketanserin by radioligand binding assay method and to compare the results with other selective 5-HT2 antagonists. The results showed that AT-1015 displayed high affinity to 5-HT2 receptors in rabbit platelet membranes. The pKi value of AT-1015 was 7.40, which is slightly lower than that of ketanserin, but higher than that of cyproheptadine. On the other hand, the displacement potency of AT-1015 for 5-HT2 receptors in rabbit platelets was similar to those of sarpogrelate and ritanserin. This is the first report of the high affinity of AT-1015 in rabbit platelets.
journal_name
Biol Pharm Bulljournal_title
Biological & pharmaceutical bulletinauthors
Rashid M,Watanabe M,Nakazawa M,Nagatomo Tdoi
10.1248/bpb.24.1188subject
Has Abstractpub_date
2001-10-01 00:00:00pages
1188-90issue
10eissn
0918-6158issn
1347-5215journal_volume
24pub_type
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