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

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Showing 91 - 100 of 107 results

Status:
Investigational
Source:
INN:nepicastat
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Nepicastat (SYN-117) is a potent and selective inhibitor of dopamine-β-hydroxylase. This compound in Phase 2 of clinical trial for the treatment cocaine addiction and posttraumatic stress disorder.
Status:
Investigational
Source:
INN:adrogolide
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Adrogolide is a chemically stable prodrug of the dopamine D1 receptor agonist A-86929. Adrogolide is rapidly converted in plasma to A-86929. A-86929 has high affinity and functional selectivity for the dopamine D1 receptor. Adrogolide has been in phase II clinical trials for the treatment of Parkinson's disease and cocaine abuse. However, this research has been discontinued. The adverse events associated with its use of adrogolide were of mild-to-moderate severity and included injection site reaction, asthenia, headache, nausea, vomiting, postural hypotension, vasodilitation, and dizziness.
Status:
Investigational
Source:
INN:adrogolide
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Adrogolide is a chemically stable prodrug of the dopamine D1 receptor agonist A-86929. Adrogolide is rapidly converted in plasma to A-86929. A-86929 has high affinity and functional selectivity for the dopamine D1 receptor. Adrogolide has been in phase II clinical trials for the treatment of Parkinson's disease and cocaine abuse. However, this research has been discontinued. The adverse events associated with its use of adrogolide were of mild-to-moderate severity and included injection site reaction, asthenia, headache, nausea, vomiting, postural hypotension, vasodilitation, and dizziness.
Status:
Investigational
Source:
INN:adrogolide
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Adrogolide is a chemically stable prodrug of the dopamine D1 receptor agonist A-86929. Adrogolide is rapidly converted in plasma to A-86929. A-86929 has high affinity and functional selectivity for the dopamine D1 receptor. Adrogolide has been in phase II clinical trials for the treatment of Parkinson's disease and cocaine abuse. However, this research has been discontinued. The adverse events associated with its use of adrogolide were of mild-to-moderate severity and included injection site reaction, asthenia, headache, nausea, vomiting, postural hypotension, vasodilitation, and dizziness.
Remacemide is a low-affinity noncompetitive NMDA receptor antagonist with sodium channel blocking properties. It has been studied for a number of conditions including acute ischemic stroke, epilepsy, Parkinsons Disease, and Huntington's disease. It was concluded, that was unlikely that remacemide would be further developed as an antiepileptic drug. As for other conditions, there no any information in the literature, why remacemide is no longer being developed for them.
Status:
Investigational
Source:
NCT02078284: Phase 1 Interventional Completed Thrombocytopenia
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



MK-212 is a 5HT2C-receptor agonist. It displays selectivity for 5-HT2C over 5-HT2A (IC50 values are 0.028 and 0.42 uM for human 5-HT2C and 5-HT2A receptors expressed in HEK293 cells respectively). A dose-dependent the effect of 5HT2C-receptor agonist MK-212 on mouse behavior was demonstrated. Intraperitoneal injection of MK-212 in high doses (0.5 and 1.0 mg/kg) increased blood level of corticosterone in mice and reduced their motor activity. In low doses of 0.1 and 0.2 mg/kg, the agonist reduced anxiety, but had no effect on motor activity. It is hypothesized that low doses of MK-212 exhibited anxiolytic activity in mice.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)



MFZ 10-7 is a high affinity negative allosteric modulator at the mGlu5 receptor (Ki = 0.67 nM). MFZ 10-7 demonstrates anxyolitic properties in mouse models. Intraperitoneal administration of MFZ 10-7 inhibited intravenous cocaine self-administration, cocaine-induced reinstatement of drug-seeking behavior and cocaine-associated cue-induced cocaine-seeking behavior in rats.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)



MFZ 10-7 is a high affinity negative allosteric modulator at the mGlu5 receptor (Ki = 0.67 nM). MFZ 10-7 demonstrates anxyolitic properties in mouse models. Intraperitoneal administration of MFZ 10-7 inhibited intravenous cocaine self-administration, cocaine-induced reinstatement of drug-seeking behavior and cocaine-associated cue-induced cocaine-seeking behavior in rats.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)



JDTic demonstrated high affinity for the kappa opioid receptor in the binding assay and highly potent and selective kappa antagonism in the [(35)S]GTP-gamma-S assay. This drug was in phase I of clinical trials for the treatment of cocaine abuse, but development was stopped because of incidence of non-sustained ventricular tachycardia.

Showing 91 - 100 of 107 results