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Irreversible interaction of beta-haloalkylamine derivatives with dopamine D1 and D2 receptors |
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| Authors: | A J Cross J L Waddington S T Ross |
| Institution: | 1. Division of Psychiatry, MRC Clinical Research Centre, Watford Road, Harrow, HA1 3UJ, U.K.;1. Smith Kline & French Laboratories, 1500 Spring Garden Street, Philadelphia, USA;1. Present address, Department of Clinical Pharmacology, Royal College of Surgeons in Ireland, Dublin 2, USA |
| Abstract: | The interaction of beta-haloalkylamine derivatives of dopamine agonists and antagonists with 3H-spiperone binding (D2 sites) and 3H-flupenthixol binding (D1 sites) was studied. N-chloroethyl derivatives of phenothiazines and thioxanthenes were potent inhibitors of the binding of both ligands. The in vitro inhibition of binding produced by these compounds was irreversible. The drugs were however only weakly active in vivo. The results suggest that beta-haloalkylamine derivatives of neuroleptics may be useful compounds for studying dopamine receptors in vitro. |
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