N-(4-trifluoromethylphenyl)amide group of the synthetic histamine receptor agonist inhibits nicotinic acetylcholine receptor-mediated catecholamine secretion
SCIE
SCOPUS
- Title
- N-(4-trifluoromethylphenyl)amide group of the synthetic histamine receptor agonist inhibits nicotinic acetylcholine receptor-mediated catecholamine secretion
- Authors
- Kim, DC; Park, YS; Jun, DJ; Hur, EM; Kim, SH; Choi, BH; Kim, KT
- Date Issued
- 2006-02-28
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Abstract
- The therapeutic targeting of nicotinic receptors requires the identification of drugs that selectively activate or inhibit a limited range of nicotine acetylcholine receptors (nAChRs). In this study, we identified N-(4-trifluoromethylphenyl)amide group of the synthetic histamine receptor ligands, histamine-trifluoromethyltoluide, that act as potent inhibitors of nAChRs in bovine adrenal chrornaffin cells. Catecholamine secretion induced by the nAChRs agonist, 1,1-dimethyl-4-phenylpiperazinium iodide (DMPP), was significantly inhibited by histamine-trifluoromethyltoluide. Real time carbon-fiber amperometry confirmed the ability of histamine-trifluoromethyltoluide to inhibit DMPP-induced exocytosis in single chromaffin cells. We also found that histamine-trifluoromethyltoluide inhibited DMPP-induced [Ca2+](i) and [Na+](i) increases, as well as DMPP-induced inward currents in the absence of extracellular calcium. Histamine-trifluoromethyltoluide had no effect on [H-3]nicotine binding or on calcium increases induced by high K+, bradykinin, veratridine, histamine, and benzoylbenzoyl ATP. Among the synthetic histamine receptor ligands, clobenpropit exhibited similarity. In addition, 4'-nitroacetanilide also significantly attenuated nAChR-mediated catecholamine secretion. In conclusion, the N-(4-trifluoromethylphenyl)amide group of the histamine-trifluoromethyltoluide might be the critical moiety in the inhibition of nAChR-mediated CA secretion. (c) 2005 Elsevier Inc. All rights reserved.
- Keywords
- catecholamine; DMPP; Ca2+ influx; histamine-trifluoromethyltoluide; nicotinic acetylcholine receptor; chromaffin cells; ADRENAL CHROMAFFIN CELLS; CENTRAL-NERVOUS-SYSTEM; PARAVENTRICULAR NUCLEUS; INTRACELLULAR CALCIUM; RELEASE; RATS; GENERATION; CHANNELS; MEDULLA; ANTINOCICEPTION
- URI
- https://oasis.postech.ac.kr/handle/2014.oak/24199
- DOI
- 10.1016/j.bcp.2005.11.021
- ISSN
- 0006-2952
- Article Type
- Article
- Citation
- BIOCHEMICAL PHARMACOLOGY, vol. 71, no. 5, page. 670 - 682, 2006-02-28
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