منابع مشابه
Molecular pharmacology and pathophysiological significance of endothelin.
Since the discovery of the most potent vasoconstrictor peptide, endothelin, in 1988, explosive investigations have rapidly clarified much of the basic pharmacological, biochemical and molecular biological features of endothelin, including the presence and structure of isopeptides and their genes (endothelin-1, -2 and -3), regulation of gene expression, intracellular processing, specific endothe...
متن کاملInternational Union of Pharmacology nomenclature of endothelin receptors.
Following the discovery of ET (Yanagisawa et a!., 1988), the existence of three distinct isoforms of ET, designated ET-1, ET-2, and ET-3, was predicted from the finding of three separate genes (Inoue et al., 1989). The expression of the three isotypes has been verified in many tissues and found to occur in various proportions. Only ET-1 is made by endothelia! cells. In addition to these endogen...
متن کاملInternational Union of Pharmacology. XXIX. Update on endothelin receptor nomenclature.
In mammals, the endothelin (ET) family comprises three endogenous isoforms, ET-1, ET-2, and ET-3. ET-1 is the principal isoform in the human cardiovascular system and remains the most potent and long-lasting constrictor of human vessels discovered. In humans, endothelins mediate their actions via only two receptor types that have been cloned and classified as the ET(A) and ET(B) receptors in th...
متن کاملPharmacology and Toxicology of Leflunomide
Leflunomide (LEF), used for rheumatoid arthritis, inhibits dihydro-orotate dehydrogenase (DHODH) and tyrosine kinase (TK) enzymes and has anti-inflammatory, lymphocyte proliferation regulatory, immunosuppression and chondroprotective effects. The most common adverse effects are gastrointestinal disorders, weight loss, hypertension, skin infection, and neurological and hematological toxicity. It...
متن کاملPharmacology of macitentan, an orally active tissue-targeting dual endothelin receptor antagonist.
Macitentan, also called Actelion-1 or ACT-064992 [N-[5-(4-bromophenyl)-6-(2-(5-bromopyrimidin-2-yloxy)ethoxy)-pyrimidin-4-yl]-N'-propylaminosulfonamide], is a new dual ET(A)/ET(B) endothelin (ET) receptor antagonist designed for tissue targeting. Selection of macitentan was based on inhibitory potency on both ET receptors and optimization of physicochemical properties to achieve high affinity f...
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ژورنال
عنوان ژورنال: Japanese Journal of Pharmacology
سال: 1991
ISSN: 0021-5198
DOI: 10.1016/s0021-5198(19)37726-1