Receptor agonists/antagonists

Receptor Agonist Antagonist Effects Gene on Chromosome... 

Localization of Receptors Agonist Antagonist Receptor Type... 

Zhang S, Qin C, Safe SH. Flavonoids as aryl hydrocarbon receptor agonists/ antagonists Effects of structure and cell context. Environ Health Perspect 2003 111 1877-82. 

Thrombin inhibitors and thrombin receptor agonists/antagonists... 

THROMBIN RECEPTOR AGONISTS/ANTAGONISTS Thrombin receptor mechanisms... 

Abstract Benzimidazole is a biologically important scaffold which displays important biological activities. Recent progress in the synthesis and bioactivity of benzimidazoles is reviewed. New synthetic procedures, including microwave-assisted synthesis, solid phase synthesis, natural product synthesis, and synthesis of bisbenzimidazoles are briefly described. Functionalization and cyclization reactions of benzimidazoles lead to a wide variety of novel benzimidazole structures. Selected bioactivity, such as anti-infective, anti-inflammatory, antitumor and receptor agonist/antagonist activities are presented. 

Fig. 2. Distribution of twelve large target-specific groups of pharmaceutical agents within the Kohonen map (a) G-protein-coupled receptors (GPCR) agonists/antagonists (5,432 compounds) (b) matrix metalloproteinase inhibitors (120 compounds) (c) tyrosine kinase inhibitors (175 compounds) (d) caspase inhibitors (50 compounds) (e) NMDA receptor agonists/antagonists (150 compounds) (f) potassium channel blockers/activators (302 compounds) ...

Rosati, R.L. and Da Silva, J.P. (1998) Discovery and predinical pharmacology of a novel, potent, nonsteroidal estrogen receptor agonist/antagonist, CP-336156, a diaryltetrahydronaphfhalene. Journal of Medicinal Chemistry, 41, 2928—2931. 

Dezocine, an opiate receptor agonist-antagonist, possessing an analgesic property (5 to 20 mg IM q. 3 to 6 hours), is used in the management of moderate to severe pain. 

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