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

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Showing 881 - 890 of 1033 results

(+)-3-(3-Hydroxyphenyl)-N-(1-propyl)piperidine ((+)-3-PPP or preclamor, (R)) is an agonist of the sigma receptors and also acts as a dopamine receptor agonist with autoreceptor as well as postsynaptic receptor stimulatory properties. In vivo experiments have shown, that preclamor, (R) inhibited DOPA accumulation in the striatum, nucleus accumbens, and medial prefrontal cortex.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)



GBR-12935 (1-{2-benzhydryloxyethyl}-4-(3-phenylpropyl)piperazine) is a potent and selective inhibitor of dopamine transporter. Gist-Brocades originally initiated studies of GBR-12935 for the treatment of cocaine dependence. Tritium-labeled GBR-12935 may be used in radioligand binding studies. GBR-12935 is considered to be the metabolite of vanoxerine, another piperazine dopamine uptake inhibitor.
SKF-83822 is a D1/D5 receptor agonist, which activates D1-like receptors coupled to stimulation of adenyl cyclase (AC), but not phosphoinositide (PI) hydrolysis. SKF-83822 is used as a tool compound to study the role of AC-coupled D1 receptors.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Dimethocaine (DMC, larocaine), a synthetic derivative of cocaine, is a widely distributed "legal high" consumed as a "new psychoactive substance" (NPS), originally was used in the 1930s as an anesthetic, primarily in dentistry, ophthalmology, and otolaryngology. This drug completely inhibits dopamine transporter and has had the potential for abuse. Dimethocaine is intended for forensic and research purposes.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)

SCH-23390 is a potent and selective antagonist of the dopamine-1 and dopamine-5 receptors (Ki = 0.2 and 0.3 nM respectively). It was found to prevent death from d-amphetamine overdose in rats and has also been investigated as a potential treatment for Parkinson's Disease and Bipolar Disorder. A single clinical trial was conducted in healthy humans where SCH-23390 induced akathisia (motor restlessness). Preclinical and clinical trials as therapeutic have been discontinued due to side-effects and lack of efficacy. However, it should be noted that a C11 radiolabeled version of the compound has been synthesized and used as a PET imaging probe for the study of Parkinson's Disease and Huntington's Disease.
Hordenine is a natural Phenethylamine compound that occurs in a number of different plants, but especially barley grass. It is structurally similar to the amino acid Tyramine. It antagonized D2-mediated beta-arrestin recruitment indicating functional selectivity. Hordenine inhibited melanogenesis by suppressing cAMP production, which is involved in the expression of melanogenesis-related proteins. Hordenine may be an effective inhibitor of hyperpigmentation. Hordenine is an indirectly acting adrenergic drug. It liberates norepinephrine from stores. In isolated organs and those structures with reduced epinephrine contents, the hordenine-effect is only very poor. Experiments in intact animals (rats, dogs) show that hordenine has a positive inotropic effect upon the heart, increases systolic and diastolic blood pressure, peripheral blood flow volume, inhibits gut movements but has no effect upon the psychomotorical behavior of mice. Hordenine is considered to be generally very safe and well-tolerated in healthy adults. Hordenine is a nootropic compound that works equally well for cognitive enhancement and athletic performance.