Effects of the monoamine stabilizer (−)-OSU6162 on locomotor and sensorimotor responses predictive of antipsychotic activity

2018 ◽  
Vol 391 (7) ◽  
pp. 761-768
Author(s):  
Vívian T. da Silveira ◽  
Jivago Röpke ◽  
Ana L. Matosinhos ◽  
Ana C. Issy ◽  
Elaine A. Del Bel ◽  
...  
Keyword(s):  
Antipsychotic Activity ◽  
Sensorimotor Responses

Design, Synthesis, Characterization, Molecular Docking, ADME Properties and In Vivo Antipsychotic Activity of Aripiprazole Related Drugs Candidates

2017 ◽  
Vol 14 (9) ◽  
Author(s):  
Selvarasu Sekar ◽  
Srinivasan Pazhamalai ◽  
Ganesan Ariharasivakumar ◽  
Mannathusamy Gopalakrishnan
Keyword(s):  
Molecular Docking ◽  
Design Synthesis ◽  
Antipsychotic Activity ◽  
Adme Properties

scholarly journals Role of mGlu2 in the 5-HT2A receptor-dependent antipsychotic activity of clozapine in mice

2018 ◽  
Vol 235 (11) ◽  
pp. 3149-3165 ◽  
Author(s):  
Kelsey S. Hideshima ◽  
Ashkhan Hojati ◽  
Justin M. Saunders ◽  
Doan M. On ◽  
Mario de la Fuente Revenga ◽  
...  
Keyword(s):  
Antipsychotic Activity

scholarly journals Correction: Chronic clozapine treatment restrains via HDAC2 the performance of mGlu2 receptor agonism in a rodent model of antipsychotic activity

2018 ◽  
Vol 44 (2) ◽  
pp. 455-456 ◽  
Author(s):  
Mario de la Fuente Revenga ◽  
Daisuke Ibi ◽  
Travis Cuddy ◽  
Rudy Toneatti ◽  
Mitsumasa Kurita ◽  
...  
Keyword(s):  
Rodent Model ◽  
Clozapine Treatment ◽  
Antipsychotic Activity ◽  
Mglu2 Receptor

SYNTHESIS AND EVALUATION OF ANTIPSYCHOTIC ACTIVITY OF 11- (4-ARYL-1-PIPERAZINYL)-DIBENZ [b,f][1,4] OXAZEPINES AND THEIR 8-CHLORO ANALOGUES

2007 ◽  
Vol 13 (2-3) ◽  
Author(s):  
B.S. Wagh† ◽  
B.P. Patil ◽  
M.S. Jain ◽  
S.S. Harak ◽  
S.B. Wagh
Keyword(s):  
Antipsychotic Activity

ChemInform Abstract: Psychotropic Agents: Synthesis and Antipsychotic Activity of Substituted β-Carbolines.

ChemInform ◽  
1987 ◽  
Vol 18 (47) ◽  
Author(s):  
M. ABOU-GHARBIA ◽  
U. R. PATEL ◽  
J. A. MOYER ◽  
E. A. MUTH
Keyword(s):  
Antipsychotic Activity ◽  
Psychotropic Agents

scholarly journals The antipsychotic activity of alcoholic extract of Withania coagulans fruits in Swiss albino mice

2018 ◽  
Vol 7 (12) ◽  
pp. 2389
Author(s):  
Amit S. Kamdi ◽  
Sarika D. Kokane ◽  
Pankaj N. Bohra ◽  
Suvarna M. Kalambe
Keyword(s):  
Avoidance Response ◽  
Conditioned Avoidance ◽  
Conditioned Avoidance Response ◽  
P Value ◽  
Alcoholic Extract ◽  
Swiss Albino Mice ◽  
Withania Coagulans ◽  
Antipsychotic Activity ◽  
Albino Mice ◽  
Cns Effects

Background: Schizophrenia is one of the most distressing central nervous system (CNS) disorders. It is described by positive, negative and cognitive symptoms. These symptoms can be controlled by the antipsychotic medicines. The numerous antipsychotic medications used today are not lacking the adverse drug reactions. The Withania coagulans a susceptible species, is not explored much for its CNS effects except in late seventies. Therefore, it was thought worthwhile to investigate anti-psychotic activities of alcoholic extract of Withania coagulans fruits. The objective of the present study was to assess the antipsychotic activity of alcoholic extract of Withania coagulans fruits in Swiss albino mice by Cook’s Pole Climb Apparatus for conditioned avoidance response (CAR)Methods: Cook’s Pole Climb Apparatus for conditioned avoidance response was used for assessing the antipsychotic activity of the alcoholic extract of 200mg/kg, 500mg/kg and 1000mg/kg doses of Withania coagulans fruits.Results: There was statistically (p-value >0.05) no significant association between any of the 200mg/kg, 500mg/kg and 1000mg/kg doses of the alcoholic extracts of Withania coagulans fruits with antipsychotic activity in Swiss albino mice.Conclusions: Withania coagulans fruits alcoholic extract did not demonstrate antipsychotic activity in Swiss albino mice under standard conditions.

scholarly journals Translational Development Strategies for TAK-063, a Phosphodiesterase 10A Inhibitor

2020 ◽  
Vol 23 (8) ◽  
pp. 524-532
Author(s):  
Thomas A Macek ◽  
Kazunori Suzuki ◽  
Karen Asin ◽  
Haruhide Kimura
Keyword(s):  
Animal Models ◽  
Healthy Subjects ◽  
Human Subjects ◽  
Phase 1 ◽  
Clinical Manifestations ◽  
Receptor Activation ◽  
Guanosine Monophosphate ◽  
Antipsychotic Activity ◽  
Dose Study ◽  
Phosphodiesterase 10A

Abstract Background TAK-063 is an inhibitor of phosphodiesterase 10A (PDE10A), an enzyme highly expressed in medium spiny neurons of the striatum. PDE10A hydrolyzes both cyclic adenosine monophosphate and cyclic guanosine monophosphate and modulates dopamine signaling downstream of receptor activation in both direct and indirect pathways of the striatum. TAK-063 exhibited antipsychotic-like effects in animal models; however, the translatability of these models to the clinical manifestations of schizophrenia and the meaningfulness for new targets such as PDE10A has not been established. Methods The TAK-063 phase 1 program included a comprehensive translational development strategy with the main objective of determining whether the antipsychotic-like pharmacodynamic effects seen in nonclinical models would translate to human subjects. To evaluate this objective, we conducted a single-rising dose study (84 healthy subjects), a positron emission tomography (PET) study (12 healthy subjects), a functional magnetic resonance imaging blood oxygen level-dependent (BOLD) study (27 healthy subjects), and a multiple-rising dose study that included people with schizophrenia (30 healthy Japanese subjects and 47 subjects with stable schizophrenia). In addition, assessments of cognition and electroencephalography (27 healthy subjects and 47 subjects with stable schizophrenia) were included. Results PDE10A engagement by TAK-063 was verified with a novel PET radiotracer for use in primates and humans. TAK-063 showed favorable pharmacokinetic and safety profiles in humans, and TAK-063 reduced ketamine-induced changes in electroencephalography and BOLD signaling in animal models and healthy human subjects. In addition, analogous effects on cognition were observed in animal models and human subjects. Conclusions Overall, the phase 1 results showed some consistent evidence of antipsychotic activity. This translational strategy may be valuable for the future development of novel therapeutic approaches, even when relevant nonclinical models are not available.

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