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

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Showing 161 - 170 of 1033 results

Status:
Investigational
Source:
INN:milenperone
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Milenperone, a dopamine receptor antagonist was studied as an antipsychotic drug. It participated in clinical trials in the management of aggressive behavior in alcoholics and epileptics. Besides, the effect of milenperone was studied for the aggressive behavior of oligophrenic patients. However, information about the further development of the drug is not available.
Status:
Investigational
Source:
INN:biriperone
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Biriperone (also known as Centbutindole) was developed as an antipsychotic drug. It has shown effective antipsychotic activity in schizophrenic patients. Biriperone acts as a dopamine antagonist, and also as a blocker of 5HT(2) receptor. Clinically the drug has passed through phase I, II & III clinical trials successfully, however, the use of this drug was banned.
Status:
Investigational
Source:
INN:etisulergine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Etisulergine (CQ 32-084) is an ergoline derivative. Etisulergine stimulates both dopamine D1- and D2-receptors, antagonizes alpha-adrenergic and serotonin 5-HT2 receptors. Etisulergine demonstrated antiparkinsonian activity in patients.
Status:
Investigational
Source:
INN:nolomirole [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Nolomirole (CHF1035) is an orally active, selective dopamine agonist, primarily activating DA2- and alpha2 receptors, thereby inhibiting norepinephrine release, which may be beneficial in heart failure. Nolomirole is able to attenuate the heart failure signs in the monocrotaline-induced congestive heart failure. CHF1035 is a mixture of two enantiomers, CHF1800 (+) and CHF1810 (-). CHF1035 and its metabolite CHF1024 significantly decreased the IOP in rabbits, and are potential novel IOP lowering agents. Especially, CHF1035 produced a substantial decrease in IOP for a prolonged period of time, and thus may prove useful in glaucoma therapy. Nolomirole is a pre-synaptic stimulator of DA2-dopaminergic and α2-adrenergic receptors in peripheral sympathetic nerve endings. These receptors act as a negative feedback mechanism, inhibiting norepinephrine secretion. In early phase clinical studies lasting 1–3 months, nolomirole reduced peripheral systemic resistance and 24 hour blood pressure and increased cardiac output. In a study of 29 patients with heart failure, followed for 10 days, a reduction in plasma norepinephrine was demonstrated. In spite of the fact that Nolomirole was in clinical trials for the treatment of heart failure, its development was discontinued.
Status:
Investigational
Source:
INN:alpiropride
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Alpiropride (RIV-2093) is a dopamine D2-receptor antagonist structurally similar to sulpiride. Alpiropride has been given orally for the treatment and prophylaxis of migraine.
Status:
Investigational
Source:
INN:cipropride
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)


Cipropride is an anti-emetic drug of the substituted benzamide class. It was discovered by Synthelabo in the early 1980s. The drug acts by blocking the dopamine receptor and thus affecting the chemo-receptor trigger zone for vomiting. Clinical trials showed that cipropride was effective for the prevention of nausea and vomiting induced by cytotoxic chemotherapy agents dacarbazine and Cis-platinum. The subsequent development of the drug was not reported.
Status:
Investigational
Source:
INN:belaperidone
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Belaperidone (LU111995) is a recently identified antipsychotic agent with high 5-hydroxytryptamine2 and dopamine D4 receptor affinities as well as D4 versus D2 receptor selectivity. The drug did not produce catalepsy. LU111995 prolongs the Q-T interval to a limited degree and is not arrhythmogenic over the physiological range of cycle lengths. Belaperidone had been in phase II clinical trials for the treatment of schizophrenia. However, the study about this drug candidate was discontinued.
Status:
Investigational
Source:
INN:lirexapride
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Lirexapride serotonin 5-HT4 receptor and dopamine D2 receptor agonists. It had been in phase II clinical trials for the treatment of irritable bowel syndrome. However, this research has been discontinued.
Status:
Investigational
Source:
INN:ciladopa
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Ciladopa, is a troponylpiperazine derivative and dopamine agonist that has been shown to influence dopaminergic mechanisms in animals. Preclinical pharmacological studies have suggested that it has antiparkinsonian activity similar to that of bromocriptine but without many of the troublesome side effects. Unfortunately in some clinical trials no significant differences was found among the treatment groups and placebo.
Status:
Investigational
Source:
INN:berupipam [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Berupipam (also known as NNC 22-0010), a dopamine antagonist with a high affinity and selectivity for D1 receptor has been studied for patients with psychotic disorders. Berupipam participated in phase I clinical trials; however, further development of this drug was discontinued