SDZ PSD 958, a novel D1 receptor antagonist with potential limbic selectivity

Autor: Markstein, R., Gull, P., Rüdeberg, C., Urwyler, S., Jaton, A. L., McAllister, K., Dixon, A. K., Hoyer, D.
Zdroj: Journal of Neural Transmission; March 1996, Vol. 103 Issue: 3 p261-276, 16p
Abstrakt: Summary SDZ PSD 958, a novel benzo[g]quinoxaline derivative exhibits the properties of a potent orally active selective D1 receptor antagonist. It has high affinity for D1-like receptors (D1, D5; pKi=9.7–9.8) labelled by [3H]SCH23390 and is at least 400 fold less active at D2-like receptors (i.e. D2, D4) labelled by [3H]spiperone. Effects in functional tests are consistent with d1 receptor antagonist properties. SDZ PSD 958 inhibited apomorphine-induced rearing in mice and prevented prolongation of novelty-induced locomotion in rats elicited by the selective D1 receptor agonist CY 208-243. By contrast, SDZ PSD 958 did not induce catalepsy and only weakly inhibited apomorphine-induced stereotyped gnawing in rats. This suggests that SDZ PSD 958 preferentially inhibits responses mediated by dopamine systems innervating the limbic system.
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