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Restrict the search for
histamine
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Status:
Investigational
Source:
USAN:ICOTIDINE [USAN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Icotidine (also known as SKF 93319) was developed as histamine H1- and H2-receptor antagonist and possessed antinociception properties. Due to its antagonist activity, was suggested that compound could have therapeutic in some inflammatory skin diseases such as the urticarias and mastocytosis.
Class (Stereo):
CHEMICAL (ACHIRAL)
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Mifentidine, a histamine H2 receptor antagonist, was studied to treat the duodenal ulcer. This drug was in phase II clinical trials when apparently further researches had been discontinued.
Status:
Investigational
Source:
INN:tecastemizole [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Tecastemizole (aka Norastemizole) is an H1 receptor antagonist that showed great promise as potential next-generation antihistamine allergy medication. Sepracor developed Norastemizole through phase III clinical trials; however, the FDA rejected the application for approval on the grounds of an unacceptable profile of adverse side-effects including phospholipidosis and cardiomyopathies in animals exposed to the drug.
Status:
Investigational
Source:
USAN:METOPRINE [USAN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Metoprine is a diaminopyrimidine folate antagonist with potential antineoplastic activity. Metoprine inhibits dihydrofolate reductase, resulting in decreased cellular folate metabolism and cell growth. Metoprine shows potent in vitro antitumor activity against several experimental tumors including methotrexate-resistant tumors. Metoprine inhibits the enzyme dihydrofolate reductase, much less effectively than methotrexate but it also inhibits histamine-N-methyltransferase, resulting in decreased histamine catabolism. S phase cells are most sensitive, whilst cells in G2 and M are least sensitive to the lethal effects of Metoprine, and a prolonged exposure to a high Metoprine concentration produces maximum cytotoxic effects. After oral administration, Metoprine has a widespread distribution and concentration in all tissues examined with the highest tissue/plasma ratios found in brain, lung, pancreas, and skin. Phase I and early Phase II clinical trials in various centers have shown activity in hypernephroma, epidermoid carcinoma arising in bronchus or head and neck, central nervous system leukemia, malignant melanoma, and mycosis fungicides. Metoprine had been in some phase II clinical trials but further studies were discontinued due to CNS and hematological toxicity.
Class (Stereo):
CHEMICAL (ACHIRAL)
Tiacrilast (also known as Ro 22-3747) is a quinazolinyl-propenoic acid derivative patented by Hoffmann-La Roche, Inc. as an antihypertensive useful for anaphylaxis management. Tiacrilast acts as a potent mast cell degranulation inhibitor in vitro and inhibits of antigen-induced histamine release from passively sensitized rat peritoneal cells in vitro. In preclinical models, Tiacrilast shows marked activity in rat passive cutaneous anaphylaxis assay, rat anaphylactic bronchospasm assay. In vitro studies have confirmed that the mechanism of action of Tiacrilast in the in vivo models is through allergic mediator release inhibition. Clinical evaluations of Tiacrilast in patients with ragweed sensitive allergic asthma, Tiacrilast demonstrates significant inhibitory activity relative to placebo in reducing acute airway responses to inhaled pollen extracts
Status:
Investigational
Source:
INN:chloropyrilene [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
