ArticleBritish journal of pharmacology2010
Mechanisms involved in the regulation of bovine pulmonary vascular tone by the 5-HT1B receptor.
Article in British journal of pharmacology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.
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2 citing papers in PubMed, 9 citations in OpenAlex.
- International Union of Basic and Clinical Pharmacology. CX. Classification of Receptors for 5-hydroxytryptamine; Pharmacology and Function.Pharmacological reviews · 2021Review
- Deletion of murine slc29a4 modifies vascular responses to adenosine and 5-hydroxytryptamine in a sexually dimorphic manner.Physiological reports · 2020Article
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4 authors at 1 institution in 1 country.
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Abstract
background and purpose5-HT(1B) receptors may have a role in pulmonary hypertension. Their relationship with the activity of BK(Ca,) a T-type voltage-operated calcium channel (VOCC) and cyclic nucleotide-mediated relaxation was examined. EXPERIMENTAL APPROACH: Ring segments of bovine pulmonary arteries were mounted in organ baths in modified Krebs-Henseleit buffer (37 degrees C) under a tension of 20 mN and gassed with 95% O(2)/5% CO(2). Isometric recordings were made using Chart 5 software. KEY
resultsContractile responses to 5-HT (10 nM-300 microM) were inhibited similarly by the 5-HT(1B) receptor antagonist SB216641 (100 nM) and the T-type VOCC blockers mibefradil (10 microM) and NNC550396 (10 microM) with no additive effect between SB216641 and mibefradil. Inhibition by SB216641 was prevented by the potassium channel blocker, charybdotoxin (100 nM). 5-HT(1B) receptor activation and charybdotoxin produced a mibefradil-sensitive potentiation of responses to U46619. Bradykinin (0.1 nM-30 microM), sodium nitroprusside (0.01 nM-3 microM), zaprinast (1 nM-3 microM), isoprenaline (0.1 nM-10 microM) and rolipram (1 nM-3 microM) produced 50% relaxation of arteries constricted with 5-HT (1-3 microM) or U46619 (30-50 nM) in the presence of 5-HT(1B) receptor activation, but full relaxation of arteries constricted with U46619, the 5-HT(2A) receptor agonist 2,5 dimethoxy-4 iodoamphetamine (1 microM) or 5-HT in the presence of 5-HT(1B) receptor antagonism. Enhanced relaxation of 5-HT-constricted arteries by cGMP-dependent pathways, seen in the presence of the 5-HT(1B) receptor antagonist, was reversed by charybdotoxin whereas cAMP-dependent relaxation was only partly reversed by charybdotoxin. CONCLUSIONS AND IMPLICATIONS: 5-HT(1B) receptors couple to inhibition of BK(Ca), thus increasing tissue sensitivity to contractile agonists by activating a T-type VOCC and impairing cGMP-mediated relaxation. Impaired cAMP-mediated relaxation was only partly mediated by inhibition of BK(Ca).
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