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Restrict the search for
dopamine
to a specific field?
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
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)
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
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.
Status:
Other
Class (Stereo):
CHEMICAL (RACEMIC)
DL-Tetrahydropalmatine (dl-THP), an active component isolated from Corydalis species (a Chinese herbal medicine). dl-THP has inhibitory effects on liver injury induced by carbon tetrachloride in mice. The drug demonstrated anxiolytic and anti-nociceptive effects in animal models. dl-THP may act through inhibition of amygdaloid dopamine release to inhibit an epileptic attack – it is a very effective anti-epileptogenic and anticonvulsant agent. dl-THP has been found to have antihypertensive effects. It acts through the 5-HT2 and/or D2-receptor antagonism in the hypothalamus to induce hypotension and bradycardia in rats.
