58038-68-9Relevant academic research and scientific papers
Antipsychotic Activity of Substituted γ-Carbolines
Abou-Gharbia, Magid,Patel, Usha R.,Webb, Michael B.,Moyer, John A.,Andree, Terrance H.,Muth, Eric A.
, p. 1818 - 1823 (2007/10/02)
Several novel substituted γ-carbolines were synthesized and examined in a series of in vitro and in vivo pharmacological tests to determine potential antipsychotic activity.Most compounds were orally active in blocking the conditioned avoidance response (CAR) in rats but did not antagonize apomorphine-induced stereotyped behavior.Compound 17 (Wy-47,384), a γ-carboline with a 3-(3-pyridinyl)propyl side chain, was selected for development as an atypical antipsychotic agent because of its potent and selective profile in preclinical psychopharmacological tests.It blocked CAR in rats with an AB50 of 14 mg/kg po, showed weak affinity for the D2 receptor site (Ki = 104 nM), and showed differential potency in antagonizing apomorphine-induced stereotyped behavior (ED50 = 11 mg/kg ip) and climbing behavior (ED50 = 4 mg/kg ip).Such activities are suggestive of antipsychotic efficacy combined with a low potential for extrapyramidal side effect (EPS) liability.
Neuroleptic Activity in 5-Aryltetrahydro-γ-carbolines
Harbert, Charles A.,Plattner, Jacob J.,Welch, Willard M.,Weissman, Albert,Koe, B. Kenneth
, p. 635 - 643 (2007/10/02)
A series of 5-aryltetrahydro-γ-carbolines was prepared by a novel N-arylation procedure and tested for neuroleptic activity in a rat antiamphetamine model.The systematic exploration of structural parameters leading to 8-fluoro-5-(4-fluorophenyl)-2-4-hydr
5-Aryl-1,2,3,4-tetrahydro-γ-carbolines
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, (2008/06/13)
2-Substituted-5-aryl-1,2,3,4-tetrahydro-γ-carbolines, their use as tranquilizing agents and the preparation thereof from 5-aryl-1,2,3,4-tetrahydro-γ-carbolines.
2-(Phenylthiopropyl)-5-aryl-1,2,3,4-tetrahydro-γ-carbolines
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, (2008/06/13)
2-(Phenylthiopropyl)-5-aryl-1,2,3,4-tetrahydro-γ-carboline tranquilizing agents and the preparation thereof from 5-aryl-1,2,3,4-tetrahydro-γ-carbolines.
