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

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Showing 91 - 100 of 993 results

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
Source:
INN:rimcazole [INN]
Source URL:

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.
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:
Investigational
Source:
INN:methoxyphedrine
Source URL:

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.
Status:
Investigational
Source:
INN:indatraline [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Indatraline (Lu 19-005) is a non-selective monoamine transporter inhibitor that has been shown to block the reuptake of dopamine, norepinephrine, and serotonin with effects similar to those of cocaine. In vivo, indatraline produced behavioral effects suggestive of enhanced dopaminergic, noradrenergic, and serotonergic activity in mice. Indatraline also substituted for a high dose of cocaine in rats trained to discriminate between a low and a high dose of cocaine, which demonstrates that indatraline produces cocaine-like discriminative stimulus effects. Indatraline has been studied to block the action of methamphetamine and MDMA.
Status:
Investigational
Source:
INN:ciclofenazine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Cyclophenazine is an antagonist of dopamine receptors, discovered by Eli Lilly. The drug is claimed to possess tranquilizing, anti-emetic action, and is able to potentiate the action of anticholinergic compounds in inhibiting the gastric secretion.
Sumanirole is a novel dopamine agonist with high affinity and efficacy at D2 dopamine receptors and has a substantial degree of selectivity for the D2 receptor over other dopamine receptor subtypes. It had been in clinical trials for the treatment of Parkinson’s disease and restless leg syndrome but these studies were terminated for the efficacy reason.
Status:
Investigational
Source:
NCT00088517: Phase 1 Interventional Completed Healthy
(2004)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT01785147: Phase 2 Interventional Completed Tobacco Addiction
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT03512171: Phase 1 Interventional Completed Healthy Adults
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)