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

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Showing 371 - 380 of 1033 results

Nafadotride is a highly potent and competitive dopamine D3 receptor antagonist (D3DR), with efficacy against D2DR and D4DR as well. Nafadotride displayed a high affinity for dopamine D2 and D3 receptors, but a low affinity for doparnine D1 and D4. At dopamine D2 and D3 receptors, the potency was concentrated on the l-enantiomer, which was 7 and 20 times, respectively, more potent than the d-enantiomer. dl-Nafadotride, l-nafadotride and d-nafadotride were 6, 10 and 2 times, respectively, more potent at dopamine D3 than at D2 receptors. As compared to haloperidol, a D 2 receptor preferring antipsychotic, the behavioral profile of nafadotride is characterized by stimulant properties on locomotor activity of rats habituated to their environment occurring at low dosage, i.e. in the range of 1 mg/kg. In contrast, nafadotride exerts typical D 2 receptor blocking responses at much higher dosage: for instance, about 100-fold higher dosages were required to observe extrapyramidal effects like catalepsy.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

GR 103691 is an effective and selective receptor antagonist of the D3DR (dopamine D3 receptor). GR 103691 was shown to have 100-fold higher selectivity for D3DR (dopamine D3 receptor) over the D2DR (dopamine D2 receptor) and D4DR (dopamine D4 receptor) sites. GR 103,691 is functionally active in vivo and will inhibit the hyperactivity response induced by intra-VTA (ventral tegmental area) injection of muscimol in rats.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)



A-412,997 or A-412997 is a highly selective agonist for the dopamine D4 receptor. In animal tests, it improved cognitive performance to a similar extent as methylphenidate, but without producing place preference or other signs of abuse liability. When dosed systemically, A-412997 crossed the blood brain barrier rapidly. It was suggested, that selective activation of the D4 receptor, A-412997, might represent a target for the treatment of attention deficit hyperactivity disorder without the potential drug abuse liability associated with current psychostimulant therapies.