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Titolo:
Inhibition of the Na,K-ATPase of canine renal medulla by several local anesthetics
Autore:
Kutchai, H; Geddis, LM;
Indirizzi:
Univ Virginia, Sch Med, Dept Mol Physiol & Biol Phys, Charlottesville, VA 22908 USA Univ Virginia Charlottesville VA USA 22908 Charlottesville, VA 22908 USA
Titolo Testata:
PHARMACOLOGICAL RESEARCH
fascicolo: 4, volume: 43, anno: 2001,
pagine: 399 - 403
SICI:
1043-6618(200104)43:4<399:IOTNOC>2.0.ZU;2-Q
Fonte:
ISI
Lingua:
ENG
Soggetto:
SYNAPTOSOMAL PLASMA-MEMBRANE; SARCOPLASMIC-RETICULUM; CA-ATPASE; LIDOCAINE; MODULATION; ENZYMES; NERVE; ALTER;
Keywords:
local anesthetics; Na+; K+-ATPase; enzyme inhibition; lidocaine; procaine; chloroprocaine; bupivacaine; mepivacaine; quaternary amines; QX-222; QX-314;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
21
Recensione:
Indirizzi per estratti:
Indirizzo: Kutchai, H Univ Virginia, Sch Med, Dept Mol Physiol & Biol Phys, Charlottesville, VA 22908 USA Univ Virginia Charlottesville VA USA 22908 ville, VA 22908 USA
Citazione:
H. Kutchai e L.M. Geddis, "Inhibition of the Na,K-ATPase of canine renal medulla by several local anesthetics", PHARMAC RES, 43(4), 2001, pp. 399-403

Abstract

The ATPase activity of Na,K-ATPase-enriched membranes from canine renal medulla was determined in the absence of local anesthetic and in the presenceof procaine, chloroprocaine, bupivacaine, mepivacaine. lidocaine, and two quaternary derivatives of lidocaine (QX-222 and QX-314) at 37 degreesC. Chloroprocaine (IC50 = 13 mM) had slightly greater potency than procaine (IC50= 17.7 mM). Bupivacaine (IC50 = 6.7 mM) was more potent than its congener mepivacaine (IC50 > 10 mM, the solubility limit). QX-222 (IC50 > 600 mM) and QX-314 (IC50 = 132 mM) had less potency than lidocaine (IC50 = 30.4 mM). This study supports the interpretation that the uncharged forms of local anesthetics are much more potent inhibitors of Na,K-ATPase activity than the cationic forms. (C) 2001 Academic Press.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 04/04/20 alle ore 08:57:52