Neuroleptic receptors: stereoselectivity for neuroleptic enantiomers

Seeman, Philip ; Westman, Karen ; Protiva, Miroslav ; Jílek, Jiri ; Jain, Padam C. ; Saxena, Anil K. ; Anand, Nitya ; Humber, Leslie ; Philipp, Adolf (1979) Neuroleptic receptors: stereoselectivity for neuroleptic enantiomers European Journal of Pharmacology, 56 (3). pp. 247-251. ISSN 0014-2999

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In order to identify a pair of neuroleptic enantiomers with the highest stereoselective interaction with neuroleptic/dopamine receptors, the effects of eight pairs of neuroleptic enantiomers were tested on the specific binding of 3H-spiperone to crude homogenates of calf caudate nucleus. The ratios of the Ki values were: (+)-butaclamol/(-)-butaclamol = 3000; dexclamol/(-)-analogue = 151; (+)-isobutaclamol/(-)-isobutaclamol = 146; (-)-CTC/(+)-CTC = 109; (-)-centbutindole/(+)-centbutindole = 20; S(+)-octoclothepin/R(-)-octoclothepin = 11. Thus, the neuroleptic receptor is highly stereoselective for the rigid butaclamol derivatives, but much less so for the flexible neuroleptics. The 3H-apomorphine binding site, however, had a stereoselectivity ratio of only 7 for isobutaclamol, further suggesting that the high affinity sites (i.e. nM) for 3H-neuroleptic binding and for 3H-apomorphine binding are different.

Item Type:Article
Source:Copyright of this article belongs to Elsevier Science.
Keywords:Butaclamol; Dopamine Receptors; Octoclothepin; Spiperone; Apomorphine
ID Code:3839
Deposited On:18 Oct 2010 09:39
Last Modified:04 Jan 2011 09:55

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