U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 61 - 70 of 311 results

Status:
Other

Class (Stereo):
CHEMICAL (RACEMIC)


ISOCLOZAPINE is typical antipsychotic that acts by blocking the receptors in the brain’s dopamine pathways. Isoclozapine has high affinities at both DA (D1 and D2) and serotonin (5-HT2A and 5-HT2C) receptors. Isoclozapine shows the greatest antipsychotic potential on inhibition of apomorphine-induced climbing in mice at quite low doses under sc or po administrations. However, Isoclozapine also produces catalepsy at low doses.
Propylnorapomorphine is a potent and selective D2 receptor agonist. Propylnorapomorphine is used as a tool compound to label dopamine receptors in rodent brain, and elicits dopaminergic behavioural effects. It stimulates motor activity, induces stereotypic behaviour and sexual stimulation. Propylnorapomorphine was investigated in clinical trial against Parkinson's disease and schizophrenia
N-Methylspiperone (NMSP) is a derivate of spiperone and high-affinity D2/3 dopamine and 5-HT2A serotonin receptor antagonist. In the biodistribution studies in rodents, there was a high accumulation of radioactivity in the liver, lung, and kidneys, whereas the brain radioactivity was not as high N-Methylspiperone is used to study the dopamine and serotonin neurotransmitter systems. Labeled with the radioisotope carbon-11, it can be used for positron emission tomography (PET). [11C] N-Methylspiperone PET is useful for objective monitoring of D2and 5-HT2A receptor occupancy and density in patients being treated with antipsychotic drugs.
(S)-SKF-83959 (MCL 201) is enantiomer of D1 receptor agonist SKF-83959. (S)-SKF-83959 is reported to be a functionally selective dopamine D1 receptor ligand with much lower affinity to dopamine D2, D3 and D5 receptors. (R)-SKF-83959 like SKF-83959, produced dose related effects on overt behavior (eye blinking) and schedule-controlled performance in squirrel monkeys. (R)-SKF-83959 increases in eye blinking and decreases in rates of fixed-ratio responding. In contrast to the effects of its S-(-) enantiomer, was relatively devoid of behavioral activity up to doses that were approximately 10-fold greater than (R)-SKF-83959.
P-88-8991 (Hydroxy Iloperidone, 4-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl] propoxy]- 3-methoxy-methylbenzenemethanol) is the major active metabolite of Iloperidone an atypical antipsychotic that used for the acute treatment of schizophrenia in adults. Metabolic reduction of Iloperidone carbonyl group leads to P-88-8991 in rats, dogs, and humans. The receptor affinity profile of P-88-8991 is comparable to that of iloperidone: this metabolite binds to the serotonin 5-HT2A receptors, adrenergic alpha1 and alpha2C receptors, and D2A receptors and with lower affinity to other monoamine (dopamine, serotonin, and histamine H1 ) receptors. The comparable receptor binding profile of P-88-8991 indicates that it is likely to contribute to the clinical profile of iloperidone. Preclinical experiments, such as the mouse apomorphine climbing test, the rat self-stimulation, and the pole climb avoidance task, indicate antipsychotic activity of P88-8991 and confirm that this metabolite crosses the blood–brain barrier