PMID: 8972718Nov 8, 1996Paper

Effect of haloperidol on the sarcoplasmic reticulum Ca-dependent adenosine triphosphatase

Biochimica Et Biophysica Acta
D Takara, Guillermo L Alonso

Abstract

Several effects of the neuroleptic agent haloperidol on the sarcoplasmic reticulum (SR) Ca-dependent adenosine triphosphatase (Ca-ATPase) and Ca transport are described. Haloperidol inhibits the Ca-ATPase activity in the presence of calcimycin. The effect depends on the conditions of preexposure of the membranes to the drug: the inhibition increases with the preincubation time; Ca and Mg protect the enzyme against the effect of the drug. The inhibitory effect of haloperidol decreases upon increasing [Ca2+], at constant [Mg], and disappears at 20 mM [Mg] for any [Ca2+], and at 0.5 mM [Ca2+] for any [Mg2+]. Haloperidol also inhibits phosphorylation of the enzyme by Pi, and ATP-dependent Ca2+ uptake, in both cases with apparent Ki = 0.10-0.15 mM, and increases the rate of Ca efflux from preloaded vesicles in this concentration range. The results suggest that haloperidol interacts with the catalytic site, interfering with the effect of the divalent catalytic cation, but not at other steps of the enzymatic cycle, where Mg2+ and Ca2+ are also activators. They are consistent with a reaction model where haloperidol interacts with the E2 conformers of the enzyme, with lower affinity for the phosphoenzyme than for the dephospho species. ...Continue Reading

References

Sep 21, 1976·Biochimica Et Biophysica Acta·P J GarrahanG L Alonso
Jan 1, 1985·Annual Review of Physiology·G Inesi
Jan 15, 1988·European Journal of Biochemistry·L De MeisA Gómez Puyou
Sep 3, 1987·Biochimica Et Biophysica Acta·B Escudero, C Gutiérrez-Merino

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Citations

Dec 24, 1997·Annals of the New York Academy of Sciences·D Takara, G L Alonso
Aug 21, 2013·Naunyn-Schmiedeberg's Archives of Pharmacology·G A SánchezD Takara
Jun 21, 2014·Naunyn-Schmiedeberg's Archives of Pharmacology·D E Di CroceD Takara
Jul 16, 2015·Naunyn-Schmiedeberg's Archives of Pharmacology·D Di CroceG A Sánchez
Nov 15, 2013·European Journal of Oral Sciences·Gabriel A SánchezDelia Takara
Sep 15, 2012·Archives of Oral Biology·Gabriel Antonio SánchezDelia Takara
Jun 26, 2004·Journal of Dental Research·G A SánchezG L Alonso

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