Tissue-specific Agonists/Antagonists

Mixed agonists/antagonists Tissue-specific agonists/ antagonists... 

Tissue-specific Agonists/Antagonists Tissue-type Plasminogen Activator T-kinin (Ile-Ser-Bradykinin)... 

Lonard DM, Smith CL (2002) Molecular perspectives on selective estrogen receptor modulators (SERMs) progress in understanding their tissue-specific agonist and antagonist actions. Steroids 67 15-24... 

Selective estrogen-receptor modulators prevent bone loss and vertebral fractures. They bind to estrogen receptors and function as tissue-specific estrogen antagonists (in breast) or agonists (in bone). 

Hf and H Receptors. Histamine exerts its actions by binding to receptors on cell membranes. Two types of histamine receptors, the Hi and H2 receptors, are known specific agonists and antagonists exist for each of these receptors. Black et al. (55) differentiated H and H2 receptors with the compounds, 2-methylhistamine and 4 methylhistamine. 2-Methylhistamine is active on tissues with H receptors 4-methylhistamine is active on tissues with H2 receptors. Classical antihistaminic drugs were developed in the 1930 s these compounds block H but not H2 receptors. Among the clinically used H -blockers are derivatives of ethanolamine, ethylenediamine, alkylamine, piperazine and phenothiazine (32). These agents are valuable in the treatment of... 

The first compound with published detailed information which supports the claims for a specific ETg antagonist is IRL 1038, (20) [Cys -Cys ] ET-1 (11-21). This compound showed specific antagonist activity both in binding assays and in endothelin-induced contraction models. With ET-3 as agonist, 3 /M IRL 1038 antagonized the ETb receptor-mediated contraction of guinea-pig ileal and tracheal smooth muscle but did not affect the ET receptor-mediated contraction of rat aortic tissue [110]. 

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