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

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Showing 11 - 20 of 60 results

Status:
Investigational
Source:
INN:butaclamol [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Butaclamol is an antipsychotic drug, which was studied for the treatment of schizophrenia. This drug has never marketed and now is used in research, because of its action as a dopamine receptor-blocking agent. Butaclamol consists of the two forms: (-)-butaclamol, an inactive drug and (+)-butaclamol, a potent neuroleptic drug.
1-(2-methoxyphenyl)piperazine is an effective blocker of striatal dopaminergic receptors in rat brain and is apparently the simplest chemical structure known to exert dopaminergic blocking activity. It is exhibited pronounced antihypertensive and weak sympatholytic activities in experimental animals. Blood pressure was also lowered in hypertensive patients and this effect was sometimes accompanied by a strong sedation, and after large repeated doses, by disorientation and stupor. In a filter paper bioassay 1-(2-methoxyphenyl)piperazine demonstrated acaricidal activity. 1-(2-methoxyphenyl)piperazine is a building block of many serotonergic and dopaminergic agents. Some of them have antidepressant activity.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Ergocornine is an ergot alkaloid. Ergocornine can inhibit prolactin release by a direct action on the anterior pituitary. It can modulate activity at both dopamine and serotonin receptors.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)



3-Tyrosine, in contrast to the para isomer, is readily racemized. The majority of the load was metabolized to m-hydroxyphenylacetic acid but m-hydroxymandelic acid and 3,4-dihydroxyphenylacetic acid were also detected. Low circulating levels of m-tyrosine in the plasma suggest that most of the load is held due to a first pass effect somewhere in the enterohepatic system and that this portion of the load is not in equilibrium with the plasma m-tyrosine. The metabolism of a m-tyrosine may give further insight into the deficiencies of the phenylalanine hydroxylating system found in the various phenotypes of phenylketonuria. 3-Tyrosine has been used experimentally as a substitute for L-DOPA in the treatment of Parkinsonism. 3-tyrosine mimics the action of Dopa in two experimental animal models. It was also obvious from the experiments with d,l- and l-m-tyrosine that only the l-isomer (3-Tyrosine) is active.
Status:
US Previously Marketed
Source:
Repoise by Robins
(1967)
Source URL:
First approved in 1967
Source:
Repoise by Robins
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Butaperazine is an antipsychotic phenothiazine. As shown in animal studies butaperazine increases striatal and mesolimbic dopamine turnover. Butaperazine is effective in the management of schizophrenia. Extrapyramidal symptoms and drowsiness are the most common adverse effects.
Status:
US Previously Marketed
First approved in 1961

Class (Stereo):
CHEMICAL (ACHIRAL)



Thiethylperazine is a antiemetic, which was used for the treatment of nausea and vomiting in patients undergoing radiotherapy, chemotherapy or as a postoperative care. Thiethylperazine exerts its therapeutic effect by blocking dopamine receptors in brain. The drug is capable of potentiating CNS depressants as well as atropine.
Promazine (Sparine) is a phenothiazine neuroleptic used for short-term management of moderate to severe psychomotor agitation and treatment of agitation and restlessness in the elderly. Promazine is an antagonist at types 1, 2, and 4 dopamine receptors, 5-HT receptor types 2A and 2C, muscarinic receptors 1 through 5, alpha(1)-receptors, and histamine H1-receptors. Promazine's antipsychotic effect is due to antagonism at dopamine and serotonin type 2 receptors, with greater activity at serotonin 5-HT2 receptors than at dopamine type-2 receptors. This may explain the lack of extrapyramidal effects. Promazine does not appear to block dopamine within the tuberoinfundibular tract, explaining the lower incidence of hyperprolactinemia than with typical antipsychotic agents or risperidone. Antagonism at muscarinic receptors, H1-receptors, and alpha(1)-receptors also occurs with promazine. Promazine is not approved for human use in the United States. It is available in the US for veterinary use under the names Promazine and Tranquazine.
Status:
US Previously Marketed
Source:
Hydergine by Sandoz
(1951)
Source URL:
First approved in 1951

Class (Stereo):
CHEMICAL (ABSOLUTE)



Dihydroergocristine is an ergot alkaloid that has an partial agonist activity on dopaminergic and alpha-adrenergic receptors and antagonist activity on serotonin receptors. The drug was approved by FDA in combination with other alkaloids (dihydroergocornine, dihydro-alpha-ergocryptine and dihydro-beta-ergocryptine mesylate salts) under the name Hydergine for the treatment of dimentia and cerebrovascular insufficiency.

Showing 11 - 20 of 60 results