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

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Showing 191 - 200 of 244 results

BAY 61-3606 is a potent inhibitor of spleen tyrosine kinase (Syk) which is playing essential roles in receptors for Fc portion of immunoglobulins and B cell receptor complex signaling in various inflammatory cells. In addition, BAY61-3606 could inhibit the inhibitor of nuclear factor kappa B kinase (IKK-alpha) kinase activity. The compound is able to inhibit neoplastic phenotype of leukemia cells as well as of colon and breast cancer cells in vitro. BAY 61-3606 also exrets antiinflammatory and antiallergic properties in animal models.
Stachydrine, a pyrrolidine betaine, was first isolated from seed husk and the pulp of the fruit of C. Leonurus, and many other Asian plants and fruits. Stachydrine is an anti-metastatic agent. Stachydrine hydrochloride induces apoptosis in MCF-7 and T47D cells and exerts inhibitory effects on proliferation by concurrently suppressing Akt and ERK survival signals, suggesting its potential efficiency in treatment of breast cancer. Stachydrine (Sta) has also been reported to possess numerous cardioprotective effects. It ameliorated pressure overload-induced diastolic heart failure by suppressing myocardial fibrosis.
(R)-Bambuterol is a selective β2-adrenoceptor agonist. R-Bambuterol Hydrochloride Tablets ("Laevo-Bambuterol") is categorized as a Class 1 new drug. Its preclinical studies show that it is more effective and have lower toxicity than Bambuterol, a popular asthma drug currenTLy on the market. Laevo-Bambuterol was approved by the China Food and Drug Administration for the treatment of asthma.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Glycodeoxycholic acid (GDCA), a bile acid, is formed in the liver from chenodeoxycholate and glycine. GDCA was one of twenty-five plasma metabolites, which were significantly different among asthma and healthy controls. Besides, GDCA was elevated in patients with acetaminophen-induced acute liver failure (AALF) and was significantly increased in non-surviving AALF patients compared with survivors. Thus GDCA level could serve as a prognostic biomarker for AALF patients.
Stachydrine, a pyrrolidine betaine, was first isolated from seed husk and the pulp of the fruit of C. Leonurus, and many other Asian plants and fruits. Stachydrine is an anti-metastatic agent. Stachydrine hydrochloride induces apoptosis in MCF-7 and T47D cells and exerts inhibitory effects on proliferation by concurrently suppressing Akt and ERK survival signals, suggesting its potential efficiency in treatment of breast cancer. Stachydrine (Sta) has also been reported to possess numerous cardioprotective effects. It ameliorated pressure overload-induced diastolic heart failure by suppressing myocardial fibrosis.
Stachydrine, a pyrrolidine betaine, was first isolated from seed husk and the pulp of the fruit of C. Leonurus, and many other Asian plants and fruits. Stachydrine is an anti-metastatic agent. Stachydrine hydrochloride induces apoptosis in MCF-7 and T47D cells and exerts inhibitory effects on proliferation by concurrently suppressing Akt and ERK survival signals, suggesting its potential efficiency in treatment of breast cancer. Stachydrine (Sta) has also been reported to possess numerous cardioprotective effects. It ameliorated pressure overload-induced diastolic heart failure by suppressing myocardial fibrosis.
Status:
US Previously Marketed
First approved in 1992

Class (Stereo):
CHEMICAL (ACHIRAL)



Nedocromil is a medication considered as mast cell stabilizer used to treat itching associated with allergic conjunctivitis. Nedocromil has been shown to inhibit the in vitro activation of, and mediator release from, a variety of inflammatory cell types associated with asthma, including eosinophils, neutrophils, macrophages, mast cells, monocytes, and platelets. Nedocromil inhibits activation and release of inflammatory mediators such as histamine, prostaglandin D2 and leukotrienes c4 from different types of cells in the lumen and mucosa of the bronchial tree. These mediators are derived from arachidonic acid metabolism through the lipoxygenase and cyclo-oxygenase pathways. The mechanism of action of nedocromil may be due partly to inhibition of axon reflexes and release of sensory neuropeptides, such as substance P, neurokinin A, and calcitonin-geneñrelated peptides. The result is inhibition of bradykinin-induced bronchoconstriction. Nedocromil does not possess any bronchodilator, antihistamine, or corticosteroid activity. Nedocromil is indicated for the treatment of itching associated with allergic conjunctivitis.
Status:
US Previously Marketed
First approved in 1992

Class (Stereo):
CHEMICAL (ACHIRAL)



Nedocromil is a medication considered as mast cell stabilizer used to treat itching associated with allergic conjunctivitis. Nedocromil has been shown to inhibit the in vitro activation of, and mediator release from, a variety of inflammatory cell types associated with asthma, including eosinophils, neutrophils, macrophages, mast cells, monocytes, and platelets. Nedocromil inhibits activation and release of inflammatory mediators such as histamine, prostaglandin D2 and leukotrienes c4 from different types of cells in the lumen and mucosa of the bronchial tree. These mediators are derived from arachidonic acid metabolism through the lipoxygenase and cyclo-oxygenase pathways. The mechanism of action of nedocromil may be due partly to inhibition of axon reflexes and release of sensory neuropeptides, such as substance P, neurokinin A, and calcitonin-geneñrelated peptides. The result is inhibition of bradykinin-induced bronchoconstriction. Nedocromil does not possess any bronchodilator, antihistamine, or corticosteroid activity. Nedocromil is indicated for the treatment of itching associated with allergic conjunctivitis.
Status:
US Previously Marketed
First approved in 1992

Class (Stereo):
CHEMICAL (ACHIRAL)



Nedocromil is a medication considered as mast cell stabilizer used to treat itching associated with allergic conjunctivitis. Nedocromil has been shown to inhibit the in vitro activation of, and mediator release from, a variety of inflammatory cell types associated with asthma, including eosinophils, neutrophils, macrophages, mast cells, monocytes, and platelets. Nedocromil inhibits activation and release of inflammatory mediators such as histamine, prostaglandin D2 and leukotrienes c4 from different types of cells in the lumen and mucosa of the bronchial tree. These mediators are derived from arachidonic acid metabolism through the lipoxygenase and cyclo-oxygenase pathways. The mechanism of action of nedocromil may be due partly to inhibition of axon reflexes and release of sensory neuropeptides, such as substance P, neurokinin A, and calcitonin-geneñrelated peptides. The result is inhibition of bradykinin-induced bronchoconstriction. Nedocromil does not possess any bronchodilator, antihistamine, or corticosteroid activity. Nedocromil is indicated for the treatment of itching associated with allergic conjunctivitis.
Status:
US Previously Marketed
First approved in 1987

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Beclometasone dipropionate or beclomethasone dipropionate is sold under the brand name Qvar among others. Beclomethasone dipropionate is a corticosteroid demonstrating potent anti-inflammatory activity. The precise mechanism of corticosteroid action on asthma is not known. Corticosteroids have been shown to have multiple anti-inflammatory effects, inhibiting both inflammatory cells (e.g., mast cells, eosinophils, basophils, lymphocytes, macrophages, and neutrophils) and release of inflammatory mediators (e.g., histamine, eicosanoids, leukotrienes, and cytokines). These anti-inflammatory actions of corticosteroids may contribute to their efficacy in asthma. Beclomethasone dipropionate is a prodrug that is rapidly activated by hydrolysis to the active monoester, 17 monopropionate (17-BMP). Beclomethasone 17 monopropionate has been shown in vitro to exhibit a binding affinity for the human glucocorticoid receptor, which is approximately 13 times that of dexamethasone, 6 times that of triamcinolone acetonide, 1.5 times that of budesonide and 25 times that of beclomethasone dipropionate. The clinical significance of these findings is unknown. Studies in patients with asthma have shown a favorable ratio between topical anti-inflammatory activity and systemic corticosteroid effects with recommended doses of QVAR. Beclometasone dipropionate was first patented in 1962 and used medically in 1972. Common side effects with the inhaled form include respiratory infections, headaches, and throat inflammation. Serious side effects include an increased risk of infection, cataracts, Cushing’s syndrome, and severe allergic reactions. Long term use of the pill form may cause adrenal insufficiency. The pills may also cause mood or personality changes. The inhaled form is generally regarded as safe in pregnancy. Beclometasone is mainly a glucocorticoid.

Showing 191 - 200 of 244 results