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2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1.
TLDR
5-(4-fluorophenyl)-2-[[4-(2-methoxyphenyl)-1-piperazinyl]methyl]pyrrole (5) is the prototype of a new class of sodium-independent dopamine D-2 antagonists, which may be particularly useful as potential antipsychotics with a low propensity to induce acute extrapyramidal side effects.
SAR study of 1-aryl-4-(phenylarylmethyl)piperazines as ligands for both dopamine D2 and serotonin 5-HT1A receptors showing varying degrees of (Ant)agonism. Selection of a potential atypical
TLDR
The syntheses of several 1-aryl-4-(arylpyridylmethylmethyl)piperazines and their affinities for dopamine D(2) and serotonin 5-HT(1A) receptors are described and the identification of the drug candidate SLV313 (4e) with equipotent and full D( 2) receptor antagonism and 5- HT( 1A) receptor agonism is identified.
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 2.
TLDR
The excellent oral activity in the apomorphine-induced climbing behavior and the conditioned avoidance response tests and the absence of catalepsy make this compound particularly promising as a potential antipsychotic with a low propensity to induce acute extrapyramidal side effects.
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