149998-17-4Relevant academic research and scientific papers
Discovery, structure-activity relationship studies, and anti-nociceptive effects of 1-phenyl-3,6,6-trimethyl-1,5,6,7-tetrahydro-4H-indazol-4-one as novel opioid receptor agonists
Cheng, Ming-Fu,Ou, Li-Chin,Chen, Shu-Chun,Chang, Wan-Ting,Law, Ping-Yee,Loh, Horace H.,Chao, Yu-Sheng,Shih, Chuan,Yeh, Shiu-Hwa,Ueng, Shau-Hua
, p. 4694 - 4703 (2014/10/15)
The μ-opioid receptor (MOR) is the major opioid receptor targeted by most analgesics in clinical use. However, the use of all known MOR agonists is associated with severe adverse effects. We reported that the 1-phenyl-3,6,6-trimethyl-1,5,6,7-tetrahydro-4H-indazol-4-ones are novel opioid receptor agonists. Subsequent structural modification resulted in the potent MOR/KOR (κ-opioid receptor) agonists 19, 20, and 21. Testing the analgesic effect of these in WT B6 mice (tail-flick test) gave ED50 values of 8.4, 10.9, and 26.6 mg/kg, respectively. The 1-phenyl-3,6,6-trimethyl-1,5,6,7- tetrahydro-4H-indazol-4-one core could be addressed in 1 or 2 synthetic steps with moderate to high percent of yield. In the adenylyl cyclase assay, compound 19 displayed a MOR/KOR agonist profile, with IC50 values of 0.73 and 0.41 μM, respectively. Current results suggest that compound 19 is a promising lead to go further development and in vitro/in vivo adverse effects studies.
TETRAHYDRO-BETA-CARBOLINES
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, (2008/06/13)
Tetrahydro-beta-carboline compounds having useful central nervous system activity are enclosed.
INTERMEDIATES TO TETRAHYDRO-BETA-CARBOLINES
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, (2008/06/13)
3-Ethanamine and 3-ethanamine related compounds are provided that are useful intermediates and have beneficial central nervous system activity.
METHOD FOR TREATING 5HT2B RECEPTOR RELATED CONDITIONS
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, (2008/06/13)
The present invention provides methods for binding a 5-HT 2B receptor in mammals using a both known and novel compounds. Further, the invention provides a method for treating or preventing 5-HT 2B related conditions. Finally, the invention provides an article of manufacture.
Tetrahydro-β-carbolines
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, (2008/06/13)
The present invention provides tetrahydro-betacarboline compounds having useful central nervous system activity.
