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

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Showing 81 - 90 of 993 results

Status:
Investigational
Source:
INN:sulverapride
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Sulverapride is a methylsulfamoylbenzamide derivative patented by Societe d'Etudes Scientifiques et Industrielles de l'Ile-de-France for the treatment of lower urinary tract disorders
Spiramide (AMI-193) is a spiperone derivative, a selective 5-HT2A, (Ki = 2 nM) 5-HT1A (Ki = 50 nM), and D2 receptor (Ki = 3 nM) antagonist, with negligible affinity for the 5-HT2C receptor (Ki = 4300 nM). The ability of Spiramide to serve as a functional 5-HT2A antagonist in behavioral studies was demonstrated through studies in which Spiramide blocked the discriminative - stimulus effects of the 5HT2A agonist 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane (DOM).
Status:
Investigational
Source:
INN:preclamol [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



(-)-3-(3-hydroxyphenyl)-N-n-propylpiperidine ((-)-3-PPP, also known as preclamol) has a dual action towards to dopamine D2 autoreceptor: it activates it and also acts concomitantly as an antagonist at postsynaptic DA receptors. It was shown, that (-)-3PPP/preclamol was a safe drug for study in the treatment of schizophrenia and may have antipsychotic efficacy. Besides, the motor effects of the drug were evaluated in nine patients with Parkinson's disease using a double-blind, placebo-controlled design. However, the small number of patients manifesting a clinically significant response and the frequently inconsistent effects could indicate that this class of agents may have relatively limited clinical utility.
Status:
Investigational
Source:
INN:tesofensine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Tesofensine (also known as NS-2330) is a novel triple monoamine reuptake inhibitor with intrinsic inhibitory activity on norepinephrine (NE), serotonin (5-HT), and dopamine (DA) transporter function. It was development by NeuroSearch as a potential therapy for Alzheimer's disease (AD) and Parkinson's diseases, but these efforts have been discontinued. In phase II clinical trials with tesofensine in obese individuals, dose-related reductions in body weight, body fat and waist circumference, as well as improvements in other obesity-related endocrine factors were observed and the FDA recently endorsed the phase III trial program for this agent.
Status:
Investigational
Source:
INN:mespiperone (¹¹C) [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Mespiperone C-11 (3-N-[11C] methylspiperone) is a radiolabeled 3-N-methylspiperone. 3-N-methylspiperone is high-affinity D2/3 dopamine and 5-HT2A serotonin receptor antagonist. It has been studied as a positron emission tomography (PET) tracer for imaging D2/3 and 5HT2A receptor densities.
Status:
Investigational
Source:
INN:manifaxine [INN]
Source URL:

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.
Status:
Investigational
Source:
INN:dopamantine
Source URL:

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.
Status:
Investigational
Source:
INN:bromerguride
Source URL:

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.