ISSN:
1432-1912
Schlagwort(e):
5-Hydroxytryptamine (5-HT, serotonin)
;
5-HT1D receptors
;
5-HT1Dβ receptors
;
Endothelial cells
;
Cyclic AMP
Quelle:
Springer Online Journal Archives 1860-2000
Thema:
Medizin
Notizen:
Abstract Pharmacological evidence has suggested the presence of 5-hydroxytryptamine (5-HT, serotonin), 5-HT1D receptors on endothelial cells but these receptors have never been identified unamiguously on this type of cells. We now report that human umbilical vein endothelial cells (HUVEC) express 5-HT1D receptors coupled to inhibitiion of cyclic AMP formatin. 5-HT and the 5-HT1D receptor agaonists 5-carboxamidotryptamine (5-CT) and sumatriptan were approximately equipotent at inhibiting forskolin-stimulated cyclic AMP accumulation in HUVEC (mean pEC50 7.6–8.2, maximal effect 30% inhibition). The 5-HT1A receptor agonist, 8-OH-DPAT was clearly less potent (pEC50 6.2) and less efficacious. The selective 5-HT1D receptor antagonist, GR127935 (1 nM) markedly inhibited the effct pf 5-HT (apparent pKB 10.8). Reverse transcription-polymerase chain reaction analysis showed the mRNA for 5-HT1Dβ receptors to be expressed in HUVEC. These results demonstrate the presence of functional 5-HT1D receptors and the expression of 5-HT1Dβreceptor mRNA in HUVEC. They support he involvement of 5-HT1Dβ receptors in endothelial-mediated responses to 5-HT.
Materialart:
Digitale Medien
URL:
http://dx.doi.org/10.1007/BF00169394
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