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Restrict the search for
m didanosine
to a specific field?
Class (Stereo):
CHEMICAL (ACHIRAL)
LAVOLTIDINE, also known as loxtidine, is a highly potent and selective histamine H2-receptor antagonist. It is a member of triazoles. It produces gastric carcinoid tumors in rodents that is why its clinical development was discontinued.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Balicatib is a potent cathepsine K inhibitor that was developed for the treatment of knee osteoarthritis. The development of Balicatib was terminated in phase II due to the occurrence of skin rashes and rarer incidences of morphea-like skin changes.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
There is no much available information related to the biological and pharmacological application of imidoline, but this compound has been found to be as potent as chlorpromazine in increasing striatal DOPA accumulation and prolactin secretion in vivo. Imidoline exhibited only weak inhibitory activity towards dopamine-sensitive adenylate cyclase and 3H-spiroperidol binding to striatal membranes in vitro. A proposed active conformation involves intramolecular hydrogen bonding between the protonated dimethylamino group and the oxygen of the imidazolidinone ring. The spatial relationship between the amine nitrogen and phenyl ring in this conformation allows proper fit of imidoline with key dimensions described for the dopamine receptor.
Status:
Investigational
Source:
INN:mazapertine [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Mazapertine (RWJ-37796) is an arylpiperazine antipsychotic with high affinity to dopamine D2 and D3, serotonin 5-HT1A and alpha 1A-adrenergic receptors. It was being studied in the treatment of schizophrenia.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Etorphine was the first potent opiate agonist employed primarily for use in non-domestic and wild species. Etorphine was 500 times as potent as morphine, with a very rapid onset and short duration of action. In morphine-dependent subjects, etorphine suppressed abstinence but for a shorter period than morphine. Etorphine is a full opiate agonist and binds to multiple opiate sites in the central nervous system. It is believed to produce its clinical effects through binding the µ-, δ-, and κ- opiate sites. It has a potent effect on depressing the respiratory centers of the CNS thus resulting in apnea being commonly seen in immobilized animals. Etorphine revolutionized the ability of biologists and veterinarians to safely capture and restrain many species that previously could not be handled. Etorphine is not currently commercially available due to lack of production by the manufacturer.
Status:
Investigational
Source:
INN:volinanserin [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Volinanserin (MDL-100,907) is a highly selective 5-HT2A receptor antagonist. It is widely used in
scientific research to investigate the function of the 5-HT2A receptor. Volinanserin is also being trialed as a
potential antipsychotic, antidepressant and treatment for insomnia. Volinanserin (M-100907) was in
phase III trials for chronic schizophrenia. In August 1999, development was discontinued for acute
schizophrenia (schizoaffective disorder) on the basis of poor results. M-100907 is also active in animal
models involving blockade of NMDA glutamatergic channel receptors, an effect known to resemble some
behavioral symptoms of schizophrenia in man. M-100907 is also claimed in other patents for the
treatment of thromboembolic disorders, for the treatment of various developmental neurological
disorders such as autism and attention deficit hyperactivity disorder.
Status:
Investigational
Source:
NCT01794104: Phase 1 Interventional Completed Neoplasm
(2013)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Indotecan (LMP400) is a novel indenoisoquinoline derivative with specific topoisomerase I inhibition activity, developed by Division of Cancer Treatment and Diagnosis National Cancer Institute for cancer treatment. In preclinical studied Indotecan inhibited the cell growth of established mouse pheochromocytoma cell lines and primary human tumor tissue cultures. Low doses of Indotecan decreased the protein levels of hypoxia-inducible factor 1 (HIF-1α), one of a family of factors studied as potential metastatic drivers in these tumors. In vitro, Indotecan showed an increase in the growth-inhibitory effects in combination with other chemotherapeutic drugs that are currently used for the treatment of pheochromocytoma. Recently Indotecan has entered Phase I clinical trials for the treatment of cancer patients at the National Cancer Institute, and definite plans are being formulated to commence Phase II clinical trials.
Class (Stereo):
CHEMICAL (ACHIRAL)
Cloperidone is a quinazolinedione derivative with sedative and antihypertensive properties. Cloperidone was discovered in 1965 by Miles Laboratories. The activity of the compound was demonstrated by behavioral observations in dogs and cats, by rotarod and activity cage experiments in mice and in other models.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Delprostenate is a synthetic analogue of PGF2-alpha, which is the naturally occurring prostaglandin used in medicine to induce labor and as an abortifacient. It is a useful synchronizer for the sheep.
Status:
Investigational
Source:
JAN:OMBRABULIN HYDROCHLORIDE [JAN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Ombrabulin is an experimental drug candidate discovered by Ajinomoto and further developed by Sanofi-Aventis for cancer treatment.
Ombrabulin is a synthetic water-soluble analog of combretastatin A4, derived from the South African willow bush (Combretum caffrum), with potential vascular-disrupting and antineoplastic activities. Ombrabulin binds to the colchicine binding site of endothelial cell tubulin, inhibiting tubulin polymerization and inducing mitotic arrest and apoptosis in endothelial cells. As apoptotic endothelial cells detach from their substrate, tumor blood vessels collapse; the acute disruption of tumor blood flow may result in tumor necrosis. Ombrabulin has been used in trials studying the treatment of Sarcoma, Neoplasms, Solid Tumor, Neoplasms, Malignant, and Advanced Solid Tumors, among others. In January 2013, Sanofi said it discontinued development of Ombrabulin after disappointing results from phase III clinical trials.
