Orally active benzamide class dopamine receptor D2/3-selective antagonist (Ki = 18 nM/D2, 22 nM/D3, 7.7 μM/D4, >10 μM/D1) with in vivo antipsychotic efficacy.
Sultopride is an orally active benzamide class dopamine receptor D2/3-selective antagonist (Ki = 18 nM/rat D2, 22 nM/human D3, 7.7 μM/human D4, >10 μM/rat D1 by competitive binding against 0.5 nM Spiperone, 0.2 nM YM-09151-2, 5 nM Spiperone, 0.2 nM SCH23390 for respective receptor) that displays in vivo antipsychotic efficacy with moderate atypical index. Sultopride exhibits little or no affinity toward 5-HT1A2/33, adrenaline receptor α1/α2, Ach receptor, histamine receptor H1, or Sigma receptors σ1/σ2. Sultopride is a racemic material composed of the highly active (-) and the less potent (+) enenatiomers.
The international journal of neuropsychopharmacology, 9(5), 539-545 (2005-11-18)
Conventional antipsychotics tend to elicit extrapyramidal symptoms at clinical doses, but dose optimization could reduce the risk of such side-effects. In-vivo receptor-binding studies have suggested that 70-80% of dopamine D2 receptor occupancy provides the desired antipsychotic effects without extrapyramidal symptoms.
Profiles of the Affinity of Antipsychotic Drugs for Neurotransmitters and Their Clinical Implications
Naunyn-Schmiedeberg's archives of pharmacology, 364(1), 81-86 (2001-08-04)
Phencyclidine (PCP)-induced head-weaving is inhibited by a novel selective sigma1-ligand, (R)-(+)-1-(4-chlorophenyl)-3-[4-(2-methoxyethyl)piperazin-1-yl]methyl-2-pyrrolidinone L-tartrate (MS-377), but not by dopamine D2 antagonists. In the present study, we examined the effects of two potent and selective sigma1-ligands, MS-377 and N,N-dipropyl-2-(4-methoxy-3-(2-phenylethoxy)phenyl) ethylamine (NE-100), on PCP-induced
The effects of the dopamine antagonists haloperidol and sultopride were investigated on the twitch response, evoked by 0.1 Hz stimulation of guinea-pig isolated ileal longitudinal muscle, and on the inhibition of the twitch response induced by 10 Hz stimulation (post-tetanic
Stereoselective blockade of cerebral dopamine receptors by sulpiride and sultopride [proceedings].
A Clow et al.
British journal of pharmacology, 67(3), 433P-433P (1979-11-01)
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