Catalogo Articoli (Spogli Riviste)

OPAC HELP

Titolo:
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
Autore:
Rashid, M; Watanabe, M; Nakazawa, M; Nagatomo, T;
Indirizzi:
Niigata Coll Pharm, Dept Pharmacol, Niigata 9502081, Japan Niigata Coll Pharm Niigata Japan 9502081 armacol, Niigata 9502081, Japan Niigata Coll Med Technol, Dept Publ Hlth, Niigata 9502076, Japan Niigata Coll Med Technol Niigata Japan 9502076 h, Niigata 9502076, Japan Niigata Univ, Fac Med, Sch Hlth Sci, Dept Med Technol, Niigata 9518518, Japan Niigata Univ Niigata Japan 9518518 t Med Technol, Niigata 9518518, Japan
Titolo Testata:
BIOLOGICAL & PHARMACEUTICAL BULLETIN
fascicolo: 10, volume: 24, anno: 2001,
pagine: 1188 - 1190
SICI:
0918-6158(200110)24:10<1188:BAOANS>2.0.ZU;2-A
Fonte:
ISI
Lingua:
ENG
Soggetto:
RECEPTOR ANTAGONIST; BLOOD PLATELETS; H-3 KETANSERIN; SMOOTH-MUSCLE; SEROTONIN; CONTRACTION; SITES;
Keywords:
AT-1015; 5-HT2 receptor; rabbit platelet;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
15
Recensione:
Indirizzi per estratti:
Indirizzo: Nagatomo, T Niigata Coll Pharm, Dept Pharmacol, 5-13-2 Kamishinei Cho, Niigata 9502081, Japan Niigata Coll Pharm 5-13-2 Kamishinei Cho Niigata Japan9502081
Citazione:
M. Rashid et al., "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", BIOL PHAR B, 24(10), 2001, pp. 1188-1190

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 [H-3]-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, buthigher 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.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 26/01/20 alle ore 16:53:03