Comparison of effects of tiapride and sulpiride on D-1, D-2, D-3 and D-4 subtypes of dopamine receptors in rat striatal and bovine caudate nucleus membranes

Japanese Journal of Pharmacology
T ArimaT Segawa

Abstract

To determine the affinity of tiapride to D-1, D-2, D-3 and D-4 subtypes of dopamine (DA) receptors, inhibitory effects of tiapride on [3H]-cis-flupenthixol, [3H]spiperone and [3H]N-propylapomorphine binding were examined in the rat striatum and bovine caudate nucleus membranes and compared to those of sulpiride and haloperidol. The IC50 values of tiapride, sulpiride and haloperidol were estimated as follows: 1440, 132 and 0.295 microM for D-1; 45.8, 8.8 and 0.004 microM for D-2; greater than 100, greater than 100 and 0.64 microM for D-3; 11.7, 2.88 and 0.0044 microM for D-4, respectively. It is suggested that the affinity of tiapride is high to D-2 and D-4, but is not high to D-1 and D-3. The affinity pattern of tiapride to each DA receptor subtype is similar to but lower than those of sulpiride and haloperidol. In the D-2 receptor assay, the IC50 values of tiapride and sulpiride were 1/22.7 and 1/19.1 of those in the presence of 100 mM NaCl, respectively, suggesting that benzamide drug binds to the D-2 subtype with higher affinity in the presence of Na+ than in the control.

References

Jan 1, 1978·The Journal of Pharmacy and Pharmacology·P JennerC D Marsden
Sep 1, 1975·European Journal of Pharmacology·B Costall, R J Naylor
Jun 1, 1980·The Journal of Pharmacy and Pharmacology·A E TheodorouC D Marsden
Jan 1, 1983·Annual Review of Neuroscience·I CreeseS E Leff
Jul 15, 1983·European Journal of Pharmacology·J Hyttel
May 8, 1981·European Journal of Pharmacology·A J Cross, J L Waddington
Aug 8, 1980·European Journal of Pharmacology·A J Cross, F Owen
Jan 1, 1984·International Journal of Developmental Neuroscience : the Official Journal of the International Society for Developmental Neuroscience·J Makihata, Y Nomura

❮ Previous
Next ❯

Related Concepts

Related Feeds

Basal Ganglia

Basal Ganglia are a group of subcortical nuclei in the brain associated with control of voluntary motor movements, procedural and habit learning, emotion, and cognition. Here is the latest research.

Antipsychotic Drugs

Antipsychotic drugs are a class of medication primarily used to manage psychosis (including delusions, hallucinations, paranoia or disordered thought), principally in schizophrenia and bipolar disorder. Discover the latest research on antipsychotic drugs here

Related Papers

Progress in Neuro-psychopharmacology & Biological Psychiatry
H ItohK Ogita
Archives of General Psychiatry
G E Crane, R A Smeets
Schizophrenia Bulletin
D V Jeste, M P Caligiuri
Archives of General Psychiatry
W S FentonT H McGlashan
© 2021 Meta ULC. All rights reserved