Binding Affinity of a Newly Synthesized 5-HT2 Antagonist, AT-1015 (N-[2-[4-(5H-Dibenzo[a, d]cyclohepten-5-ylidene)-piperidino]ethyl]-1-formyl-4-piperidinecarboxamide Monohydrochloride Monohydrate), in the Rabbit Platelet Membrane

Mamunur RASHID; Masatomo WATANABE; Mikio NAKAZAWA; Takafumi NAGATOMO

doi:10.1248/bpb.24.1188

Notes

Binding Affinity of a Newly Synthesized 5-HT₂ Antagonist, AT-1015 (N-[2-[4-(5H-Dibenzo[a, d]cyclohepten-5-ylidene)-piperidino]ethyl]-1-formyl-4-piperidinecarboxamide Monohydrochloride Monohydrate), in the Rabbit Platelet Membrane

Mamunur RASHID, Masatomo WATANABE, Mikio NAKAZAWA, Takafumi NAGATOMO

著者情報

キーワード: AT-1015, 5-HT₂ receptor, rabbit platelet

ジャーナルフリー

2001 年 24 巻 10 号 p. 1188-1190

DOI https://doi.org/10.1248/bpb.24.1188

詳細

抄録

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 pK_i 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.

責任著者(Corresponding author)

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