clozapine and propizepine

clozapine has been researched along with propizepine* in 2 studies

Other Studies

2 other study(ies) available for clozapine and propizepine

Article	Year
The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds. Bioorganic & medicinal chemistry letters, 2014, Jan-15, Volume: 24, Issue:2 Compounds 7, 8, and 9, derived from the novel scaffolds 3, 5, and 6, were synthesized and evaluated in vitro. The b,c→c,d shift of the E-phenyl ring resulted in a large decrease (ca. 20- to 1000-fold) in binding to the 5-HT2A, 5-HT2C and H2, receptors, and a modest decrease (ca. 10- to 20-fold) in binding to the 5-HT5A, D2, D5, and α1D, receptors. The b,c→d,e shift resulted in a large decrease in binding to the 5-HT1D, 5-HT2C, 5-HT6, and H1 receptors, a modest decrease in binding to 5-HT1A, 5-HT5A and D2, D5, α2B, and H2 receptors, and a large increase in affinity to the 5-HT3, 5-HT6, and σ1 receptors. Topics: Benzodiazepinones; Isomerism; Protein Binding; Protein Structure, Tertiary; Receptors, Cell Surface	2014
Effects of JL13, a pyridobenzoxazepine with potential atypical antipsychotic activity, in animal models for schizophrenia. The Journal of pharmacology and experimental therapeutics, 2001, Volume: 298, Issue:1 JL13 [5-(4-methylpiperazin-1-yl)-8-chloro-pyrido[2,3-b][1,5] benzoxazepine fumarate] is a substance with a close structural resemblance to clozapine. However, it is less sensitive to oxidation and may therefore have less hematological side effects. In the present study, JL13 was compared with clozapine and haloperidol in several animal models for schizophrenia. The paw test represents a screening model for antipsychotic drugs that can discriminate between drugs with extrapyramidal side effects and drugs without. Haloperidol increased both forelimb retraction time and hindlimb retraction time (HRT), whereas both clozapine and JL13 increased only HRT. In the prepulse inhibition paradigm, all three drugs reversed the apomorphine- and the amphetamine-induced disruption of prepulse inhibition. However, whereas haloperidol was equally effective against both dopaminergic drugs, JL13 and clozapine were more effective against amphetamine. Finally, only JL13 was able to increase prepulse inhibition in normal rats, whereas only clozapine reduced basal startle amplitude. Taken together, these data suggest that JL13 may be an effective antipsychotic drug, with a profile similar to clozapine. Topics: Amphetamine; Animals; Antipsychotic Agents; Benzodiazepinones; Central Nervous System Stimulants; Clozapine; Disease Models, Animal; Drug Evaluation, Preclinical; Haloperidol; Locomotion; Male; Pyridines; Rats; Rats, Wistar; Reflex, Startle; Schizophrenia	2001

Article

Year

The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds.

Bioorganic & medicinal chemistry letters, 2014, Jan-15, Volume: 24, Issue:2

Compounds 7, 8, and 9, derived from the novel scaffolds 3, 5, and 6, were synthesized and evaluated in vitro. The b,c→c,d shift of the E-phenyl ring resulted in a large decrease (ca. 20- to 1000-fold) in binding to the 5-HT2A, 5-HT2C and H2, receptors, and a modest decrease (ca. 10- to 20-fold) in binding to the 5-HT5A, D2, D5, and α1D, receptors. The b,c→d,e shift resulted in a large decrease in binding to the 5-HT1D, 5-HT2C, 5-HT6, and H1 receptors, a modest decrease in binding to 5-HT1A, 5-HT5A and D2, D5, α2B, and H2 receptors, and a large increase in affinity to the 5-HT3, 5-HT6, and σ1 receptors.

Topics: Benzodiazepinones; Isomerism; Protein Binding; Protein Structure, Tertiary; Receptors, Cell Surface

2014

Effects of JL13, a pyridobenzoxazepine with potential atypical antipsychotic activity, in animal models for schizophrenia.

The Journal of pharmacology and experimental therapeutics, 2001, Volume: 298, Issue:1

JL13 [5-(4-methylpiperazin-1-yl)-8-chloro-pyrido[2,3-b][1,5] benzoxazepine fumarate] is a substance with a close structural resemblance to clozapine. However, it is less sensitive to oxidation and may therefore have less hematological side effects. In the present study, JL13 was compared with clozapine and haloperidol in several animal models for schizophrenia. The paw test represents a screening model for antipsychotic drugs that can discriminate between drugs with extrapyramidal side effects and drugs without. Haloperidol increased both forelimb retraction time and hindlimb retraction time (HRT), whereas both clozapine and JL13 increased only HRT. In the prepulse inhibition paradigm, all three drugs reversed the apomorphine- and the amphetamine-induced disruption of prepulse inhibition. However, whereas haloperidol was equally effective against both dopaminergic drugs, JL13 and clozapine were more effective against amphetamine. Finally, only JL13 was able to increase prepulse inhibition in normal rats, whereas only clozapine reduced basal startle amplitude. Taken together, these data suggest that JL13 may be an effective antipsychotic drug, with a profile similar to clozapine.

Topics: Amphetamine; Animals; Antipsychotic Agents; Benzodiazepinones; Central Nervous System Stimulants; Clozapine; Disease Models, Animal; Drug Evaluation, Preclinical; Haloperidol; Locomotion; Male; Pyridines; Rats; Rats, Wistar; Reflex, Startle; Schizophrenia

2001