Pharmacological evidence for a functional serotonin-2B receptor in a human uterine smooth muscle cell line

The Journal of Pharmacology and Experimental Therapeutics
Curtis R Kelly, Najam A Sharif

Abstract

The present study investigated the serotonin-induced increase in phosphoinositide hydrolysis and mobilization of intracellular Ca2+ ([Ca2+]i) in human uterine smooth muscle cells (HUSMCs) to identify the serotonergic receptor positively coupled to phospholipase C in these cells. In phosphoinositide (PI) assays, serotonin (5-HT) and alpha-methyl-5-HT were potent, full agonists (EC50 = 20 and 4.1 nM, respectively), whereas the phenylethylamine, R-(-)-1-(4-iodo-2,5-dimethoxyphenyl)-2-aminopropane hydrochloride, was less active (EC50 = 63 nM). Proposed 5-HT2B-selective agonists, BW-723C86 [alpha-methyl-5-(2-thienylmethoxy)-1H-indole-3-ethanamine hydrochloride] and (+)-norfenfluramine, exhibited strong agonist potency and efficacy comparable with 5-HT (EC50 = 18 and 33 nM, respectively) and approximately 15-fold more potency than (-)-norfenfluramine (EC50 = 500 nM). 5-HT2C receptor agonists m-chlorophenylpiperazine and MK-212 [6-chloro-2-(1-piperaxinyl)pyrazine] were weak agonists in these cells, with potencies of 110 and 880 nM, respectively. A similar rank order of potency was observed in [Ca2+]i mobilization assays (r = 0.9, p < 0.005) in the HUSMC and with contraction of rat stomach fundus strips that contain a 5-HT2B receptor (...Continue Reading

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Citations

Nov 19, 2013·Journal of Ocular Pharmacology and Therapeutics : the Official Journal of the Association for Ocular Pharmacology and Therapeutics·Najam A SharifDorette Ellis
Oct 28, 2008·European Journal of Pharmacology·Tatsuro NakamuraTetsuro Taneike
Sep 9, 2008·International Journal of Gynaecology and Obstetrics : the Official Organ of the International Federation of Gynaecology and Obstetrics·Annalisa PieralliMassimiliano Fambrini
Jun 4, 2014·Comparative Biochemistry and Physiology. Toxicology & Pharmacology : CBP·Alla Edward LychkovaLuigi Michele Pavone
Sep 27, 2016·European Journal of Obstetrics, Gynecology, and Reproductive Biology·Nilgun GurbuzBulent Ozpolat
Oct 11, 2016·International Journal of Obstetric Anesthesia·H LiX M Lin
Jun 20, 2008·Reproductive Sciences·Yolande CordeauxGordon C S Smith
Jan 26, 2018·Journal of Ocular Pharmacology and Therapeutics : the Official Journal of the Association for Ocular Pharmacology and Therapeutics·Ya Fatou Njie-MbyeNaj Sharif
Jan 25, 2018·Journal of Ocular Pharmacology and Therapeutics : the Official Journal of the Association for Ocular Pharmacology and Therapeutics·Sunny E OhiaNaj A Sharif
Feb 26, 2014·Pharmacological Reviews·Chase H BourkeMichael J Owens
Dec 17, 2008·The Journal of Pharmacology and Experimental Therapeutics·Yolande CordeauxGordon C S Smith
Feb 10, 2007·Journal of Biomolecular Screening·Kelly J CassuttWeimin Tang

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