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Titolo:
The antidepressant imipramine inhibits the M-type K+ current in rat sympathetic neurons
Autore:
Cuellar-Quintero, JL; Garcia, DE; Cruzblanca, H;
Indirizzi:
Univ Nacl Autonoma Mexico, Fac Med, Dept Fisiol, Mexico City 04510, DF, Mexico Univ Nacl Autonoma Mexico Mexico City DF Mexico 04510 y 04510, DF, Mexico Univ Colima, Ctr Univ Invest Biomed, Colima 28045, Mexico Univ Colima Colima Mexico 28045 Univ Invest Biomed, Colima 28045, Mexico
Titolo Testata:
NEUROREPORT
fascicolo: 10, volume: 12, anno: 2001,
pagine: 2195 - 2198
SICI:
0959-4965(20010720)12:10<2195:TAIITM>2.0.ZU;2-V
Fonte:
ISI
Lingua:
ENG
Soggetto:
PHOSPHOLIPASE-C; G-PROTEINS; CHANNELS; CALCIUM; RELEASE; SUPPRESSION; RECEPTORS; PATCHES;
Keywords:
antidepressant drugs; imipramine; M-current regulation; neurons; potassium channels;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
17
Recensione:
Indirizzi per estratti:
Indirizzo: Cruzblanca, H Univ Nacl Autonoma Mexico, Fac Med, Dept Fisiol, AP 70250, Mexico City 04510, DF, Mexico Univ Nacl Autonoma Mexico AP 70250 Mexico CityDF Mexico 04510
Citazione:
J.L. Cuellar-Quintero et al., "The antidepressant imipramine inhibits the M-type K+ current in rat sympathetic neurons", NEUROREPORT, 12(10), 2001, pp. 2195-2198

Abstract

This study aimed to assess the effects of the antidepressant drug imipramine (IMI) on the neuronal M-type K+ current (I-K(M)) We show that IMI reversibly reduces I-K(M) with an IC50 of 7 muM The V-0.5 and slope factor of thesteady state activation curve remained unchanged after IMI, indicating a mode of action that is voltage insensitive for blocking the M-channel. Patchpipette application of IMI elicits same inhibitory response suggesting a binding site on the M-channel accessible from both sides of the cell membrane. Accordingly, the inhibitory effect of IMI is larger by rising external pH near to the pK(a) of the drug. Therefore, we propose that a neutral form of IMI binds more efficiently to M-channels to exert its inhibitory action by a voltage-independent mechanism. NeuroReport 12:2195-2198 (C) 2001 Lippincott Williams & Wilkins.

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Documento generato il 25/11/20 alle ore 17:32:39