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Restrict the search for
alpha-tocopherol
to a specific field?
Status:
Investigational
Source:
INN:tasipimidine [INN]
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Class (Stereo):
CHEMICAL (ABSOLUTE)
Atilmotin (also known as BAX-ACC-1638), a motilin receptor agonist, is short acting, with t1/2 less than 10 min. It was shown that at doses of 6, 30 or 60 mg intravenously, it affected esophageal, lower esophageal sphincter (LES), and gastric motility. LES and gastric pressures were increased, whereas there was disruption of esophageal peristalsis characterized by lower amplitude and failed contractions. The drug can have the clinical implementation for stomach motility disorders but is needed further study.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Meluadrine (Hoku 81) is a beta-adrenergic receptor agonist with tocolytic activity. Meluadrine binds to and activates beta-2 adrenergic receptors of myometrial smooth muscle in the uterus, thereby activates adenyl cyclase, an enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cAMP). Increased cAMP levels leads to a reduction in intracellular calcium concentration, thereby causes smooth muscle relaxation and decreases the intensity of uterine contractions. Meluadrine is a bronchodilator, and one of the metabolites of tulobuterol. Meluadrine was approximately 8 times more potent than tulobuterol, approximately twice as potent as salbutamol, and approximately as potent as isoprenaline in relaxing effect on the isolated tracheal smooth muscle preparation of guinea pigs.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Securinine is a plant-derived alkaloid from the Securinega plant that has been used clinically as a therapeutic for primarily neurological related diseases. Securinine is well-known GABAA antagonist and recently it was found that Securinine is able to up-regulate p53 protein and to modulate the related family member p73 protein in a p53-dependent fashion, inducing p73 in the HCT116 p53(-) cells and down-regulating it in the p53(+) cells. Securinine induces G1 phase cell cycle arrest, upregulates expression of p53 and Bax, and downregulates expression of Bcl-2, PI3K, mTOR, and p70s6k in breast cancer cells and promyelocytic leukemia cells. Securinine activates p38 MAPK, enhancing monocyte antibacterial activity in vitro as well. This compound also exhibits antimicrobial activity against Alternaria, Curvularia, and Helminthosporum. Additionally, securinine decreases AChE activity and suppresses amyloid-β (Aβ)-induced glial inflammatory responses in animal models of Alzheimer’s disease, improving cognitive deficits. Securinine’s activity as a GABA antagonist, likely explains its reported clinical success in limited studies for the treatment of neurological conditions such as amyotrophic lateral sclerosis (ALS), poliomyelitis and multiple sclerosis. Securinine has not been utilized in the United States, it has been used clinically in several other countries particularly China and Russia. In China, it is considered one of the 50 fundamental Chinese herbs and is used in Chinese herbal medicine.
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Belarizine was studied as a cerebral vasodilator.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Status:
Investigational
Source:
NCT01904318: Phase 1 Interventional Completed Healthy
(2013)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Source:
INN:carfloglitazar [INN]
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
ALFETAMINE (aletamine) is an antidepressant and analgesic. The pharmacologic activity profile of aletamine closely resembles that of the tricyclic antidepressants imipramine and amitriptyline. Effects shared are antagonism of RO4-1284-induced ptosis and depressed exploratory behavior, depression of spontaneous motor activity, prolongation of hexobarbital hypnosis and anticonvulsant action in mice, hypotension and potentiation of norepinephrine pressor effects in dogs, antimuricidal effects, hypothermia in rats and local anesthesia in rabbits and guinea pigs. Aletamine differed from imipramine and amitriptyline as follows: (1) aletamine exerted no apparent central or peripheral anticholinergic effect as suggested by lack of influence on tremorine-induced tremors or salivation; (2) although aletamine was less potent on a milligram basis than imipramine and amitriptyline in preventing RO4-1284 depression, aletamine was more potent than imipramine in counteracting existing reserpine depression (ptosis, depressed exploratory behavior) in mice. Amitriptyline was inactive against reserpine depression. The pharmacologic effects of aletamine differ in several respects from those of d-amphetamine. The effects of aletamine on spontaneous motor activity, hexobarbital hypnosis and body temperature in rodents and on blood pressure in dogs are in opposite direction to those of amphetamine. In further contrast to amphetamine, grouping of mice has no influence on the toxicity of aletamine. Aletamine does not appear to be an inhibitor of monoamine oxidase in vivo since it does not enhance tryptamine-induced convulsions in rats.
