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

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Showing 241 - 250 of 305 results

Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)



SB-271046 is one of the first selective 5-HT6 receptor antagonists to be discovered. SB-271046 is a potent, selective and orally active 5-HT6 receptor antagonist with a pKi value of 8.9. This compound provides a useful tool for further elucidating the physiological function of 5-HT6 receptors in vivo. SB-271046 was found to increase levels of the excitatory amino acid neurotransmitters glutamate and aspartate, as well as dopamine and noradrenaline in the frontal cortex and hippocampus of rats, and 5-HT6 antagonists have been shown to produce nootropic effects in a variety of animal studies. Suggested applications of SB-271046 included treatment of schizophrenia and other psychiatric disorders. A phase I clinical development of SB-271046 by GlaxoSmithKline (GSK) was discontinued due to a poor BBB permeability.
3-Methoxytyramine (3-MT) is a human trace amine that occurs as a metabolite of the neurotransmitter dopamine. It has been shown to act as an agonist of human TAAR1, and an inhibitor of mitochondrial respiration. 3-MT has garnered research interest for its potential links and implications to Parkinson's disease and other Neurological disorders.
Anabasine, a tobacco alkaloid, was used as a biomarker of active tobacco use. Anabasine is a selective alpha7-nicotinic acetylcholine receptor agonist. Anabasine antagonized MK-801-elicited mouse popping behavior, an animal model of schizophrenia.
Anabasine, a tobacco alkaloid, was used as a biomarker of active tobacco use. Anabasine is a selective alpha7-nicotinic acetylcholine receptor agonist. Anabasine antagonized MK-801-elicited mouse popping behavior, an animal model of schizophrenia.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Piperidine is a normal constituent in mammalian brain. It was shown to affect synaptic mechanism in the CNS, and influence neural mechanisms governing regulation of emotional behavior, sleeping, and extrapyramidal function. In addition, there are enzyme systems within the brain that synthesize and metabolize piperidine, and uptake and storage mechanisms for piperidine are found in the nerve endings. Piperidine, which proved to be a highly effective “antipsychotomimetic” agent in rats, has been reported to bring about substantial improvement in a variety of schizophrenic patients.
PHA-543613 was discovered by Pfizer and has been under development primarily as a potential treatment of schizophrenia. PHA-543613 acts as an agonist to the Neuronal acetylcholine receptor protein alpha-7 subunit. A single human trial was conducted in healthy human volunteers, but the compound has been studied extensively in rat models for schizophrenia as well as Parkinson's disease and Alzheimer's disease.
Propylnorapomorphine is a potent and selective D2 receptor agonist. Propylnorapomorphine is used as a tool compound to label dopamine receptors in rodent brain, and elicits dopaminergic behavioural effects. It stimulates motor activity, induces stereotypic behaviour and sexual stimulation. Propylnorapomorphine was investigated in clinical trial against Parkinson's disease and schizophrenia
Status:
US Previously Marketed
First approved in 1970

Class (Stereo):
CHEMICAL (MIXED)



Mesoridazine (brand name Serentil) is a phenothiazine antipsychotic. It was marketed in the U.S. for the treatment of schizophrenia, behavioral problems in mental deficiency and chronic brain syndrome, alcoholism and psychoneurotic symptoms, such as anxiety and tension. Due to the risk of serious cardiac events the indicated use of Serentil was limited to severely ill schizophrenic patients who fail other therapies. Based upon animal studies, mesoridazine acts indirectly on reticular formation, whereby neuronal activity into reticular formation is reduced without affecting its intrinsic ability to activate the cerebral cortex. Mesoridazine shows a moderate adrenergic blocking activity in vitro and in vivo and antagonizes 5-hydroxytryptamine in vivo.
Status:
US Previously Marketed
First approved in 1963

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Carfenazine (brand name Proketazine) is an antipsychotic and tranquilizer of the phenothiazine group. It is used in the treatment of acute or chronic schizophrenic reactions in hospitalized patients. Proketazine blocks postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the brain; depresses the release of hypothalamic and hypophyseal hormones and is believed to depress the reticular activating system thus affecting basal metabolism, body temperature, wakefulness, vasomotor tone, and emesis. The following is a list of possible side effects that may occur from all constituting ingredients of Proketazine: akathisia, tardive dyskinesia, extrapyramidal symptoms, allergic purpura.
Status:
US Previously Marketed
Source:
Cydril by Tutag
(1961)
Source URL:
First approved in 1957
Source:
Levonor by Nordmark (Purdue Frederick)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



LEVAMFETAMINE the levorotatory form of amphetamine. L-amphetamine, is a central nervous system (CNS) stimulant known to increase wakefulness and concentration in association with decreased appetite and fatigue. Pharmaceuticals that contain levoamphetamine are currently indicated and prescribed for the treatment of attention deficit hyperactivity disorder (ADHD), obesity, and narcolepsy in some countries. L-Amphetamine succinate was sold in Hungary between 1952 and 1955 under the brand name Cydril.

Showing 241 - 250 of 305 results