当前位置： SCI文献检索 > EUROPEAN JOURNAL OF PHARMACOLOGY期刊下所有文献 > Identification of [3H]P1075 binding sites and P1075-activated K+ currents in ovine choroid plexus cells.

Identification of [3H]P1075 binding sites and P1075-activated K+ currents in ovine choroid plexus cells.

Abstract：

:This study examined the pharmacological characteristics of binding sites for the potent K+ channel opener [3H]P1075, as well as the functional effects of P1075 on ionic currents and membrane potential, in ovine choroid plexus (OCP) cells. [3H]P1075 bound to OCP cells with a Kd of 26 +/- 4 nM and a Bmax of 10400 +/- 480 sites/cell. Labelled sites were stereoselective and inhibited by potassium channel openers with a rank order of potency: P1075 > BMS-182264, ((4-[[9cyanoimino)[(1,2,2-trimethylpropyl)amino]-methyl]amino]benz onitrile) > pinacidil > nicorandil > diazoxide. The K(ATP) channel antagonist glyburide inhibited [3H]P1075 binding with a Ki of 2 microM. The presence of K(ATP) channels on OCP cells was examined by patch clamp and fluorescent (membrane-potential sensitive dye) techniques. In some cells, P1075 activated an outward potassium current which was blocked by glyburide. P1075 produced a glyburide-sensitive, concentration-dependent, hyperpolarization of OCP cells. Levcromakalim hyperpolarized more strongly than its 3R,4S enantiomer, BRL 38226 ((3R-trans)-3,4-dihydro-3-hydroxy-2,2-dimethyl-4-(2-oxo-1-pyrrolidinyl)- 2H-1-benzopyran-6-carbonitrile) indicating a stereoselective interaction. These data indicate that epithelial OCP cells contain glyburide-sensitive K(ATP) channels.

journal_name

Eur J Pharmacol

journal_title

European journal of pharmacology

authors

Dickinson KE,Baska RA,Cohen RB,Bryson CC,Smith MA,Schroeder K,Lodge NJ

doi

10.1016/s0014-2999(97)01617-8

subject

Has Abstract

pub_date

1998-03-12 00:00:00

pages

97-101

issue

1

eissn

0014-2999

issn

1879-0712

pii

S0014-2999(97)01617-8

journal_volume

345

pub_type

杂志文章

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