Výsledky vyhledávání - "J D, Leander"

m-CPP hypolocomotion is selectively antagonized by compounds with high affinity for 5-HT2C receptors but not 5-HT2A or 5-HT2B receptors

Autor: H E Shannon, D L Nelson, V L Lucaites, Scott D. Gleason, J D Leander

Publikováno v: Behavioural Pharmacology. 12:613-620

The ability of m-CPP [1-(m-chlorophenyl)piperazine] to produce hypolocomotion is well documented. This effect has been postulated to be due to activation of the 5-HT(2C) receptor. It is only recently that the tools necessary to clearly delineate whic

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c48230b1843ae8ddc7192ee0a019a3ce
https://doi.org/10.1097/00008877-200112000-00005

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The discriminative stimulus properties of LY233708, a selective serotonin reuptake inhibitor, in the pigeon

Autor: Mary C. Wolff, J. D. Leander

Publikováno v: Psychopharmacology. 146:275-279

Rationale: Understanding the contribution of the various serotonin (5-HT) receptor subtypes to the behavioral effects of selective serotonin reuptake inhibitors (SSRIs) may contribute to the discovery of increasingly effective drugs for the treatment

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::022c82fcff11d27a78dedeb62ab414ba
https://doi.org/10.1007/s002130051117

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Structure−Activity Studies of 6-(Tetrazolylalkyl)-Substituted Decahydroisoquinoline-3-carboxylic Acid AMPA Receptor Antagonists. 1. Effects of Stereochemistry, Chain Length, and Chain Substitution

Autor: Macklin Brian Arnold, Paul L. Ornstein, D D Schoepp, J. D. Leander, Charles Willis Lugar, Peter Stanley Borromeo, David Lodge, N. K. Allen, Thomas J. Bleisch

Publikováno v: Journal of Medicinal Chemistry. 39:2219-2231

A series of 6-substituted decahydroisoquinoline-3-carboxylic acids were prepared as excitatory amino acid (EAA) receptor antagonists. These compounds are antagonists at the N-methyl-D-aspartate (NMDA) and 2-amino-3-(5-methyl-3-hydroxyisoxazol-4-yl) p

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::94a405526c3761a60a97c8fb39e531c5
https://doi.org/10.1021/jm950912p

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(3SR,4aRS,6SR,8aRS)-6-(1H-Tetrazol-5-yl)decahydroisoquinoline-3-carboxylic Acid, a Novel, Competitive, Systemically Active NMDA and AMPA Receptor Antagonist

Autor: Paul L. Ornstein, David Lodge, Macklin Brian Arnold, Darryle Darwin Schoepp, Joseph P. Tizzano, N. K. Allen, J. D. Leander

Publikováno v: Journal of Medicinal Chemistry. 38:4885-4890

We report the synthesis and characterization of 6 (LY246492), which is a competitive N-methyl-D-aspartate (NMDA) and 2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propanoic acid (AMPA) receptor antagonist. Tetrazole-substituted amino acid 6 was prepared

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ccfcd4403607e1bb2bdf67f4c7305a9d
https://doi.org/10.1021/jm00025a005

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Comparison of the antiemetic effects of a 5-HT1A agonist, LY228729, and 5-HT3 antagonists in the pigeon

Autor: J D Leander, Mary C. Wolff

Publikováno v: Pharmacology Biochemistry and Behavior. 52:571-575

Vomiting may be induced by a variety of agents such as drugs, oncolytics, and provocative motion, as well as being conditioned to occur to environmental stimuli. Such emesis has recently been shown to be blocked by agonists at the 5-HT1A subtype of s

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::305715fb76c4ef38e50f6d0afc8051a2
https://doi.org/10.1016/0091-3057(95)00142-j

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Discovery of a Potent, Peripherally Selective trans-3,4-Dimethyl-4-(3-hydroxyphenyl)piperidine Opioid Antagonist for the Treatment of Gastrointestinal Motility Disorders

Autor: Darryle Darwin Schoepp, Buddy E. Cantrell, J. S. Gidda, Dennis M. Zimmerman, J. D. Leander, B G Johnson

Publikováno v: Journal of Medicinal Chemistry. 37:2262-2265

Structure-activity relationship studies were pursued within N-substituted-trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines in an effort to discover a peripherally selective opioid antagonist with high activity following systemic administration. Alte

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::81b5e69bdcbb57290260d230f90eb356
https://doi.org/10.1021/jm00041a003

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3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity

Autor: Laurane G. Mendelsohn, B G Johnson, A E Takemori, J D Leander, W N Shaw, J D Snoddy, Jon K. Reel, David T.W. Wong, Buddy E. Cantrell, Charles H. Mitch

Publikováno v: Journal of Medicinal Chemistry. 36:2842-2850

A series of (3R*,4R*)-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists with varying substituents on the nitrogen were evaluated for their effect on food consumption in obese Zucker rats. Opioid affinity (mu, kappa, and delta for selected

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::22faa681e06223eecbccf3101cfbb93a
https://doi.org/10.1021/jm00072a002

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