Elsevier

Neuroscience Letters

Volume 71, Issue 2, 11 November 1986, Pages 224-228
Neuroscience Letters

HR 375: A potential antipsychotic drug that interacts with dopamine D2 receptors and σ-receptors in the brain

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Abstract

The potential antipsychotic HR 375 (3-(4-(3-(4-fluorobenzoyl)-propyl-piperazino-l-yl-isoquinolino-hydrochloride) inhibited [3H]spiperone binding to dopamine D2 receptors and (+)-[3H]SKF-10047 binding to σ-receptors. The drug was, however, almost inactive in phencyclidine and μ-, κ- and δ-opioid receptor binding assays. HR 375 inhibited binding of (+)-[3H]SKF-10047 to σ-sites in a competitive manner. The dissociation constant of (+)-[3H]SKF-10047 binding to σ-receptors was increased from 62 nM (47–91 nM) to 263 nM (204–370 nM) in the presence of 33 nM HR 375. The number of binding sites (Bmax) was, however, not affected. It is concluded that the pharmacological properties of HR 375, at least in part, may be attributable to its interaction with σ-receptors.

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