Lin CH, Lee YM, Sheu JR, Cheng CY, Chang MJ and Yen MH |
------>authors3_c=None ------>paper_class1=1 ------>Impact_Factor=None ------>paper_class3=2 ------>paper_class2=1 ------>vol=57 ------>confirm_bywho=yangyuan ------>insert_bywho=??? ------>Jurnal_Rank=None ------>authors4_c=None ------>comm_author=0 ------>patent_EDate=None ------>authors5_c=None ------>publish_day=None ------>paper_class2Letter=None ------>page2=322 ------>medlineContent= ------>unit=E0200 ------>insert_date=19991209 ------>iam=1 ------>update_date= ------>author=??? ------>change_event=5 ------>ISSN=None ------>authors_c=None ------>score=500 ------>journal_name=Pharmacology ------>paper_name=Pharmacological characteristics of MJ-451, a new benzopyran-derived ATP-sensitive potassium channel opener, in guinea-pig isolated trachea. ------>confirm_date=20000518 ------>tch_id=085007 ------>pmid=9792972 ------>page1=314 ------>fullAbstract=In this study, we determined the pharmacological activities of MJ-451 (6-cyano-3S,4R-dihydro-2, 2-dimethyl-2H-3-hydroxy-4-[2-oxo-5S-1-hydroxmethyl)-1-pyrrolidinyl ]-1 -benzopyran) in guinea pig isolated trachea and compared its effects with those of cromakalim. MJ-451 (0.1-10 micromol/l) and cromakalim (0.01-1 micromol/l) produced concentration-dependent relaxation of guinea pig isolated trachea precontracted with carbachol (0.5 micromol/l) or histamine (1 micromol/l). MJ-451 (0.03-30 micromol/l), as well as cromakalim (0.03-30 micromol/l), caused a complete and concentration-dependent relaxation of guinea pig isolated trachea precontracted with 20 mmol/l KCl, but did not inhibit the spasmogenic effect of 80 mmol/l KCl. However, theophylline (30-3,000 micromol/l) caused a complete and concentration-dependent relaxation of guinea pig isolated trachea precontracted with either 20 or 80 mmol/l KCl. Propranolol (0.1 micromol/l) markedly antagonized the relaxant action of isoprenaline, but not that of MJ-451 in carbachol-contracted isolated trachea. 8-(p)-sulfophenyltheophylline (150 micromol/l), a selective P1 purinoceptor antagonist, had no effect against the tracheal relaxation induced by MJ-451, but markedly depressed the concentration-response curve of 5~-N-ethylcarboxamidoadenosine. Charybdotoxin (10 micromol/l), a large-conductance Ca2+-activated K+ channel blocker, failed to modify the relaxant activity of MJ-451 in carbachol-contracted isolated trachea. The ATP-sensitive K+ channel blocker, glibenclamide (0.1, 1 and 10 micromol/l) concentration-dependently antagonized the relaxant activity of MJ-451 in carbachol-contracted isolated trachea. It is concluded that MJ-451 is a selective ATP-sensitive K+ channel opener in the tracheal smooth muscle of the guinea pig. ------>tmu_sno=None ------>sno=605 ------>authors2=None ------>authors3=None ------>authors4=None ------>authors5=None ------>authors6=None ------>authors6_c=None ------>authors=Lin CH, Lee YM, Sheu JR, Cheng CY, Chang MJ and Yen MH ------>delete_flag=0 ------>SCI_JNo=None ------>authors2_c=None ------>publish_area=None ------>updateTitle=Pharmacological characteristics of MJ-451, a new benzopyran- derived ATP-sensitive potassium channel opener, in guinea pig isolated trachea. ------>language= ------>check_flag=0 ------>submit_date= ------>country=None ------>no= ------>patent_SDate=None ------>update_bywho= ------>publish_year=1998 ------>submit_flag= ------>publish_month=None |