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

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Showing 291 - 300 of 993 results

Status:
Other

Class (Stereo):
CHEMICAL (RACEMIC)

(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.
SKF83959 is a benzodiazepine derivative which acts as an agonist of D1 receptor. Activation of D1 receptors by SKF83959 fails to stimulate adenylyl cyclase and inhibits the stimulation of adenylyl cyclase induced by dopamine but stimulates phosphatidylinositol 4,5-biphosphate hydrolysis in membranes of frontal cortex. SKF83959 was identified as a specific agonist for the heteromer D1/D2 complex. SKF83959 elicit anti-parkinsonism effects in monkeys and rodents. In lower concentrations, SKF83959 inhibits serotonin, norepinephrine and dopamine transporters and is an allosteric regulator of sigma 1 receptor. The compound has demonstrated activity in a preclinical model of depression.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Nitracaine, a new psychoactive substance, a structural analog of the dopamine reuptake inhibitor, dimethocaine; intended for research applications. The physiological and toxicological properties of this compound are still not known.