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Restrict the search for
dopamine
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Class (Stereo):
CHEMICAL (ACHIRAL)
Elopiprazole [DU 29894 or 1-(7-benzofuranyl)-4-[[5-(4-fluorophenyl)-1-H-pyrrol-2yl]methyl]piperazine) is an antagonist at dopamine D2 and D3 receptors and an agonist at serotonin1A receptors. Elopiprazole development for the treatment of psychotic disorders has been discontinued.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Manifaxine (GW 320659) is a highly selective neuronal norepinephrine and dopamine re-uptake inhibitor. It has been in phase II clinical trials by GlaxoSmithKline for the treatment of attention deficit hyperactivity disorder and obesity. Manifaxine development has been discontinued.
Status:
Investigational
Source:
INN:tefludazine [INN]
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Tefludazine (Lu 18-012) is a mixed D2 and 5-HT2 receptor antagonist that was developed as a potential antipsychotic compound. It was shown that tefludazine induced a dose-dependent decrease in both nigra pars compacta (SNC) and ventral tegmental area (VTA) dopamine (DA) activity. The development of the drug was discontinued in Phase I due to toxicological findings in dogs.
Status:
Investigational
Source:
INN:clotixamide [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Clothixamide is a dopamine antagonist. The compound was invented by Pfizer in the 1960s and is claimed to be useful for the chemotherapy of mental diseases and especially for the control of excited states. Also, clothixamide is claimed to have potent antiemetic properties.
Class (Stereo):
CHEMICAL (ACHIRAL)
Dopamantine is the adamantine derivative. It combined elements of both amantadine and dopamine in its structure, shares some pharmacological effects of amantadine. Dopamantine is the anti-Parkinson drug, which has passed clinical trials. Dopamantine showed a high activity against Plasmodium berghei parasites that cause malaria.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Bromerguride is an ergot derivative with dopamine antagonistic activity. Bromerguride has been claimed to bind to 5-HT1A receptors and to have 5-HT agonist properties. The neuropharmacological effects caused by the drug in animals were characterized by a central depressant neuroleptic-like symptomatology; the neuroleptic activity of the Bromerguride being at least in the same order of magnitude as haloperidol.
Status:
Investigational
Source:
NCT00295724: Phase 3 Interventional Completed Chronic Low Back Pain
(2005)
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Bicifadine (DOV-220075) is not a narcotic and is well-tolerated and, in preclinical studies, has been shown not to act at any opiate receptor, but inhibits monoamine neurotransmitter uptake by recombinant human transporters in vitro with a relative potency of norepinephrine:serotonin:dopamine of 1:2:17. Bicifadine was in Phase II clinical trial for pain caused by diabetic neuropathy, in addition, was in phase III clinical trial to treat Chronic Low Back Pain, but that studies were discontinued
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Rimcazole is a carbazole derivative that acts as a sigma receptor antagonist and studied as potential antipsychotic agent for the treatment of acute schizophrenic patients. In open-clinical trials Rimcazole (BW 234U) appears to be effective in acute schizophrenic patients. However, subsequent clinical trials demonstrated that rimcazole lacked efficacy in schizophrenic patients and it is now primarily used as an experimental tool. In addition to its actions as receptor antagonist, rimcazole also has high affinity for dopamine transporters, and inrecent years it has served as a lead compound for the development of novel dopamine transporter ligands.
Status:
Investigational
Source:
NCT03781128: Phase 2 Interventional Recruiting Cluster Headache
(2019)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Lysergide (LSD) is a semi-synthetic hallucinogen and is one of the most potent drugs known. Recreational use became popular between the 1960s to 1980s, but is now less common. LSD was first synthesized by Albert Hoffman while working for Sandoz Laboratories in Basel in 1938. Some years later, during a re-evaluation of the compound, he accidentally ingested a small amount and described the first ‘trip’. During the 1950s and 1960s, Sandoz evaluated the drug for therapeutic purposes and marketed it under the name Delysid®. It was used for research into the chemical origins of mental illness. Recreational use started in the 1960s and is associated with the ‘psychedelic period’. LSD possesses a complex pharmacological profile that includes direct activation of
serotonin, dopamine and norepinephrine receptors. In addition, one of its chief sites of
action is that of compound-specific (“allosteric”) alterations in secondary messengers
associated with 5HT2A and 5HT2C receptor activation and changes in gene expression.
The hallucinogenic effects of LSD are likely due to agonism at 5HT2A and 5HT2C
receptors. LSD is also an agonist at the majority of known
serotonin receptors, including 5HT1A, 5HT1B, 5HT1D, 5HT5A, 5HT6 and 5HT7 receptors. During the 1960s, LSD was investigated for a variety of psychiatric indications, including the following: as an aid in treatment of schizophrenia; as a means of creating a "model psychosis"; as a direct antidepressant; and as an adjunct to psychotherapy. LSD is listed in Schedule I of the United Nations 1971 Convention on Psychotropic Substances.
Status:
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Methoxyphedrine (para-methoxymethcathinone, 4-methoxymethcathinone, bk-PMMA, PMMC, Methedrone, 4-MeOMC) is a phenethylamine, amphetamine, and cathinone derivative that acts as a triple reuptake/release/reversible monoamine oxidase inhibitor and used as a recreational drug. Methedrone has been found to be a potent serotonin transporter (SERT) and norepinephrine transporter (NET) inhibitor, but a weak dopamine transporter (DAT) inhibitor. Methedrone induces the transportation mediated release of NE, DA, and 5-HT from cells preloaded with monoamines making it a serotonin-norepinephrine-dopamine (SNDRA) releasing agent, also known as triple releasing agent (TRA), which is a common characteristic among drugs of abuse. The health risks associated with Methedrone are unknown but are expected to be similar to other cathinones. The deaths of two young men in southeast Sweden in 2009 were attributed to Methedrone overdose.