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Restrict the search for
alpha-tocopherol acetate
to a specific field?
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
Procymate is a cyclohexylpropyl derivative patented by Compagnie Francaise des Matieres Colorantes as a non-hypnogenic depressor of the nervous system.
Class (Stereo):
CHEMICAL (ACHIRAL)
Cirazoline is an agonist of alpha1A adrenergic receptor, a partial agonist of alpha1B and alpha1D receptors, and an antagonist of alpha2 adrenergic receptors. Cirazoline was used to study the biologic function of adrenergic receptors. Injection of cirazoline into to the paravenricular hypothalamic nucleus of rats suppressed food and water intake. Cirazoline caused a large renal vasopressor response in rats. Systemic administration of cirazoline impaired spatial working memory in monkeys.
Status:
Investigational
Source:
NCT00756782: Phase 2 Interventional Withdrawn Advanced Hepatocellular Carcinoma
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Amsilarotene (TAC-101) is a retinobenzoic acid (RAR) derivative with high affinity to the RAR-alpha receptor. It is a Retinoic acid receptor alpha antagonist. Amsilarotene is an orally absorbed synthetic retinoid. This analogue of
vitamin A (retinol) binds to nuclear retinoic acid receptor-a
(RAR-a), activates RAR-a transcriptional activity, and has
shown antitumor activity in primary and metastatic preclinical
models of liver cancer. Amsilarotene inhibits retinoblastoma-gene product (RB) phosphorylation and increases the presence of 2 cyclin-dependent kinase (CDK) inhibitors, resulting in cell cycle arrest. This agent also causes a cytotoxic decline in cyclin A and thymidylate synthase expression.Amsilarotene inhibits tumor growth in
the liver with low toxicity and markedly improves survival in
both primary HCC and metastatic colon cancer models. It was in phase II clinical development with Taiho Pharmaceutical for liver cancer, however it was discontinued.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Enalkiren (A-64662) is a potent, dipeptide renin inhibitor, mimics the transition state of the human renin substrate, angiotensinogen. The results of clinical trials with enalkiren suggest that renin inhibitors may be safe, useful therapeutic agents in the management of hypertension. In addition, it exerts intraocular pressure lowering pressure. Enalkiren development for the treatment of glaucoma, heart failure, hypertension has been discontinued.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Ecalcidene (1-[(1alpha,3beta,5Z,7E,20S)-1,3-dihydroxy-24-oxo-9,10-secochola-5,7,10(19)-trien-24-yl]-piperidine) is a 1-hydroxyvitamin D analogue. Ecalcidene was being developed by Barrier Therapeutics as an oral therapy for psoriasis and acne. However, development has been discontinued.
Class (Stereo):
CHEMICAL (ACHIRAL)
Lusaperidone (R107474) is a potent and relatively selective alpha(2)-adrenoceptor antagonist. It was under clinical evaluation for the treatment of depression, characterized by anergia and lack of drive. However, further clinical development has been stopped. Radiolabeled lusaperidone may be used as a potential radioligand for studying alpha(2)-adrenoceptors using PET.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Codoxime is a synthetic derivative of an opiate dihydrocodeinone. It differs from dihydrocodeinone by the substitution of a carboxymethyl oxime for the ketonic oxygen at carbon 6 of the dihydrocodeinone molecule. Codoxime has been proposed as an antitussive with prolonged duration of action. In a clinical trial conducted on prisoner volunteers in 1966, it was found that codoxime has a capacity to produce physical dependence of the morphine type.
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.
