- PYRIDINONE ANTAGONISTS OF ALPHA-4 INTEGRINS
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The present invention provides compounds that are alpha4 integrin antagonists having a structure according to the following formula (I) or a tautomer, mixture of tautomers, salt or solvate thereof, wherein Cy, ring A, m, n, p, R1, R2
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Page/Page column 89-90
(2010/11/17)
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- BENZODIOXOLE, BENZOFURAN, DIHYDROBENZOFURAN, AND BENZODIOXANE MELATONERGIC AGENTS
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Novel derivatives of benzodioxa alkylene ethers are provided which are useful as melatonergic agents.
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Page/Page column 22
(2010/02/09)
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- Nonneurotoxic Tetralin and Indian Analogues of 3,4-(Methylenedioxy)amphetamine (MDA)
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Four cyclic analgues of the psychoactive phenethylamine derivative 3,4-(methylenedioxy)amphetamine were studied.These congeners, 5,6- and 4,5-(methylenedioxy)-2-aminoindan (3a and 4a, respectively), and 6,7- and 5,6-(methylenedioxy)-2-aminotetralin (3b and 4b, respectively) were tested for stimulus generalization in the two-lever drug-discrimination paradigm.Two groups of rats were trained to discriminate either LSD tartrate (0.08 mg/kg) from saline, or (+/-)-MDMA*HCl (1.75 mg/kg) from saline.In addition, a 2-aminoindan (5a) and 2-aminotetralin (5b) congener of the hallucinogenic amphetamine 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane (DOM) were also evaluated.None of the methylenedioxy compounds substituted in LSD-trained rats, while both 3a and 3b fully substituted in MDMA-trained rats.Compounds 4a and 4b did not substitute in MDMA-trained rats.Compounds 5a and 5b did not substitute in MDMA-trained rats, although 5a substituted in LSD-trained rats, but with relatively low potency compared to its open-chain counterpart.In view of the now well-established serotonin neurotoxicity of 3,4-(methylenedioxy)amphetamine and its N-methyl homologue 1, 3a and 3b were evaluated and compared to 1 for similar toxic effects following a single acute dose of 40 mg/kg sc.Sacrifice at 1 week showed that neither 3a nor 3b depressed rat cortical or hippocampal 5-HT or 5-HIAA levels nor were the number of binding sites (Bmax) depressed for paroxetine.By contrast, and in agreement with other reports, 1 significantly depressed all three indices of neurotoxicity.These results indicate that 3a and 3b have acute behavioral pharmacology similar to 1 but that they lack similar serotonin neurotoxicity.
- Nichols, David E.,Brewster, William K.,Johnson, Michael P.,Oberlender, Robert,Riggs, Robert M.
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p. 703 - 710
(2007/10/02)
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