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Restrict the search for
dopamine
to a specific field?
Status:
Investigational
Source:
INN:seproxetine [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Seproxetine, also known as (S)-norfluoxetine, is a selective serotonin reuptake inhibitor (SSRI). It is the most important active metabolite of the widely used antidepressant fluoxetine, but little is known about its pharmacological actions. Seproxetine was being investigated by Eli Lilly and Company as an antidepressant; however, a cardiac side effect was noted and development was discontinued.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Sarizotan (also known as EMD-128,130), a chromane derivative that was developed as a selective 5-HT1A receptor agonist and D2 receptor antagonist. Experiments on animal models have shown that the drug effectively suppressed levodopa-induced dyskinesia in primate and rodent models of Parkinson's disease, and tardive dyskinesia in a rodent model. Sarizotan participated in phase II/III clinical trials in the treatment of dyskinesia associated with the dopaminergic treatment of Parkinson's disease. However, further development for this disease was discontinued by Merk, because phase III did not confirm earlier Phase II findings. On July 14, 2015, Newron Pharmaceuticals, research, and development company focused on the novel central nervous system (CNS) and pain therapies, announced that the U.S. Food and Drug Administration (FDA) has granted Orphan Drug Designation to sarizotan for treatment of Rett syndrome. Besides, the drug now is an ongoing clinical trial phase II/III to investigate its the tolerability and efficacy in reducing respiratory abnormalities in Rett Syndrome.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Radafaxine (GW353162, ( )-(2S,3S)-2-(3-chlorophenyl-3,5,5-trimethyl-2-morphinol) or S,S-hydroxybupropion) is an active metabolite of bupropion. It acts as an inhibitor of the dopamine transporter. Radafaxine was investigated for the treatment of depression however, development was discontinued.
Status:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Aplindore (DAB-452) is a small molecule that displays potent dopamine D2 receptor partial agonist activity in in vitro and in vivo assays and is predicted to have antipsychotic efficacy without motor side effects. Aplindore had been in phase II clinical trials for the treatment of Parkinson's disease and restless legs syndrome. Aplindore was generally well tolerated and there were no withdrawals due to adverse events and no serious adverse events.
Class (Stereo):
CHEMICAL (RACEMIC)
Cliropamine (D 16427) is a positive inotropic compound.
Status:
Investigational
Source:
INN:zicronapine [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Zicronapine (formerly known as Lu 31-130), an oral antipsychotic that was studied for the treatment of schizophrenia. The drug was used in a phase III clinical trial.
Status:
Investigational
Source:
INN:amitifadine [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Amitifadine is a novel, serotonin-preferring triple reuptake inhibitor with a relative potency to inhibit serotonin (5-HT), norepinephrine (NE), and dopamine (DA) reuptake. Amitifadine is most potent against the 5-HT transporter. Amitifadine did not cause marked inhibition of major CYP450 isoenzymes, and had a good safety margin at the hERG ion channel. Initial clinical trial in patients with severe major depression demonstrated significant antidepressant activity with amitifadine, including attenuating symptoms of anhedonia, and a tolerability profile that was comparable to placebo. Amitifadine did not increase any sexual side effects as well as weight gain. It’s in phase III clinical trial for the treatment of Major depressive disorder.
Class (Stereo):
CHEMICAL (ACHIRAL)
Fananserin is a potential antipsychotic compound with a high affinity for both D4 and 5-HT2A receptors, and negligible affinity for D2 receptors. Fananserin has been researched for the treatment of schizophrenia. Fananserin was the first selective D4/5-HT2A antagonist to undergo clinical trials for schizophrenia. It has a high affinity for D4 (Ki 2.9 nM) and 5-HT2A (Ki 0.37 nM) receptors and is over 100-fold selective versus H1, a1 adrenergic, 5-HT1A and D2 dopamine receptors. Development of this compound was halted following
phase II clinical trials due to lack of efficacy.
Status:
Investigational
Source:
INN:carmoxirole [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Carmoxirole is a dopamine D2 receptor agonist with limited central activity that modulates sympathetic activation and subsequently reduces pre-load and afterload in animals. It was shown, that carmoxirole induced beneficial effects on hemodynamic and neurohumoral parameters in heart failure. In addition, experimental evidence showed that carmoxirole lowered blood pressure in various models of hypertension mainly or exclusively through inhibition of noradrenaline release from sympathetic nerve endings. That effect of carmoxirole was mediated by presynaptic dopamine receptors with the characteristic that release inhibition was restricted to low rates of sympathetic nerve discharge.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Sonepiprazole exhibits highly specific binding
to the D4 dopamine receptor with more than 100-fold
selectivity for the D4 receptor over other receptors, including
dopamine, serotonin, and adrenergic receptors. It is a neutral antagonist at the D4 dopamine
receptor and is devoid of dopamine agonist activity. Sonepiprazole selectively induces c-fos expression in
the prefrontal cortex and blocks behavioral, biochemical, and
genomic effects of repeated amphetamine administration in rats. Sonepiprazole was investigated as an antipsychotic for the treatment of schizophrenia in a placebo-controlled clinical trial, but in contrast to its comparator olanzapine no benefits were found and it was not researched further for this indication.
