- COMPOUNDS, COMPOSITIONS AND METHODS FOR TREATING NASH, NAFLD, AND OBESITY
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The present technology relates to methods of treating NASH, NAFLD and/or obesity using compounds of Formulas I, II, III, IV, V, and/or VI. The methods include administering to a subject suffering from one or more of non-alcoholic steatohepatitis (NASH), non- alcoholic fatty liver disease (NAFLD) and/or obesity a therapeutically effective amount of such a compound
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Paragraph 00249
(2021/04/10)
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- New halogenated tris-(phenylalkyl)amines as h5-HT2Breceptor ligands
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A series of compounds in which various halogen substituents were incorporated into a phenyl ring of a tris-(phenylalkyl)amine scaffold, was synthesized and evaluated for affinity to h5-HT2receptors. In general, all compounds were found to have
- Kapadia, Nirav,Ahmed, Shahrear,Harding, Wayne W.
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supporting information
p. 3216 - 3219
(2016/07/12)
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- Identification of tris-(phenylalkyl)amines as new selective h5-HT2B receptor antagonists
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A series of tris-(phenylalkyl)amines was synthesized and evaluated for affinity to human 5-HT2 receptors. In general, the compounds displayed high affinity (4 of 11 analogs had Ki values 2B receptor vs. other 5-HT2 receptors. Functional assays revealed that the compounds are 5-HT2B antagonists. This journal is
- Ponnala, Shashikanth,Kapadia, Nirav,Harding, Wayne Wesley
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supporting information
p. 601 - 605
(2015/04/27)
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- Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine
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The naturally occurring aporphine alkaloid nantenine, has been shown to antagonize behavioral and physiological effects of MDMA in mice. We have synthesized (±)-nantenine via an oxidative cyclization reaction with PIFA and evaluated its binding profile against a panel of CNS targets. To begin to understand the importance of the chiral center of nantenine with regards to its capacity to antagonize the effects of MDMA in vivo, (R)- and (S)-nantenine were prepared and evaluated in a food-reinforced operant task in rats. Pretreatment with either nantenine enantiomer (0.3 mg/kg ip) completely blocked the behavioral suppression induced upon administration of 3.0 mg/kg MDMA. (±)-Nantenine displayed high affinity and selectivity for the α1A adrenergic receptor among several other receptors suggesting that this α1 subtype may be significantly involved in the anti-MDMA effects of the enantiomers.
- LeGendre, Onica,Pecic, Stevan,Chaudhary, Sandeep,Zimmerman, Sarah M.,Fantegrossi, William E.,Harding, Wayne W.
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scheme or table
p. 628 - 631
(2010/06/19)
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- CORYDALINE DERIVATIVES USEFUL FOR REDUCING LIPID LEVELS
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The present technology relates to compounds of Formulas (V) and (VI) and methods of making and using such compounds. Methods of use include prevention and treatment of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, hepatic steatosis, and metabolic syndrome. Compounds disclosed herein also lower total cholesterol, LDL- cholesterol, and triglycerides and increase hepatic LDL receptor expression, inhibit PCSK9 expression, and activate AMP-activated potein kinase.
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Page/Page column 88
(2010/07/09)
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- COMPOUNDS, COMPOSITIONS AND METHODS FOR REDUCING LIPID LEVELS
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Compositions comprising extracts or isolated or purified compounds from plants of the genus Corydalis provide prevention and treatment of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, hepatic steatosis, and metabolic syndrome. Corydalis compounds and their derivatives of natural and synthetic origins lower total cholesterol, LDL-cholesterol, and triglycerides and increase hepatic LDL receptor expression and activate AMP-activated protein kinase. Specific stereoisomers of Corydalis compounds with lipid lowering activity include 14R-(+)-corypalmine, 14R,13S-(+)-corydaline, 14R-(+)-tetrahydropalmatin, (+)-corlumidin, d-(+)-bicuculline, and (+)-egenine.
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Page/Page column 39
(2009/03/07)
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