Pharmacologic characterization of contractile serotonergic receptors in human isolated mesenteric artery
Journal of Cardiovascular Pharmacology, cilt.41, sa.2, ss.307-315, 2003 (Scopus)
- Yayın Türü: Makale / Tam Makale
- Cilt numarası: 41 Sayı: 2
- Basım Tarihi: 2003
- Doi Numarası: 10.1097/00005344-200302000-00021
- Dergi Adı: Journal of Cardiovascular Pharmacology
- Derginin Tarandığı İndeksler: Scopus
- Sayfa Sayıları: ss.307-315
- Anahtar Kelimeler: 5-hydroxytryptamine, characterization, sumatriptan, 5-HT1B/1D receptors, 5-HT2A receptors, human mesenteric artery
- Sağlık Bilimleri Üniversitesi Adresli: Evet
Özet
The 5-hydroxytryptamine (5-HT) receptors mediating contraction in human isolated mesenteric arteries were characterized. Endothelium-denuded human isolated mesenteric arteries were used. 5-HT induced concentration-dependent contractions in mesenteric arteries (Emax, 127.37 ± 7.61% of 80 mM KCl maximal contraction; pD2, 6.73 ± 0.09 [-logEC50]). Sumatriptan, a selective 5-HT1B/1D receptor agonist, induced concentration-dependent contractions in some of the arteries (Emax, 61.82 ± 10.04%; pD2, 6.56 ± 0.21, n = 9) but not in the others (Emax < 5%, n = 13), suggesting that functional 5-HT1B/1D receptors exist in some but not in all mesenteric arteries. GR127935 (a selective 5-HT1B/1D receptor antagonist, 3 nM) inhibited sumatriptan-induced contractions in arteries in which sumatriptan responses were strong in an insurmountable manner. GR127935 (10 nM) also inhibited 5-HT responses and shifted the concentration-response curve of 5-HT to the right significantly (p < 0.05; pD2s were 6.54 ± 0.18 and 5.93 ± 0.11 in the presence of vehicle and GR127935, respectively). Ketanserin (0.01-1 μM) competitively antagonized 5-HT responses in human mesenteric arteries: pA2 value was 8.40 ± 0.25 (slope of Schild regression, 1.43 ± 0.18; r2, 0.98). Tropisetron (5-HT3 receptor antagonist) and prazosin (α1-adrenoceptor antagonist) did not affect the contractions induced by 5-HT. These results suggest that 5-HT2A and 5-HT1B/1D receptors, but not 5-HT3 and α1-adrenoceptors, are involved in the 5-HT-induced contractions in human isolated mesenteric arteries. Sumatriptan-induced and 5-HT1B/1D receptor-mediated responses vary greatly among patients.