Search Results - "McElroy, John F"
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Peripheral Cannabinoid-1 Receptor Inverse Agonism Reduces Obesity by Reversing Leptin Resistance
Published in Cell metabolism (08-08-2012)“…Obesity-related leptin resistance manifests in loss of leptin’s ability to reduce appetite and increase energy expenditure. Obesity is also associated with…”
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Behavioral and Pharmacological Validation of the Gerbil Forced-Swim Test: Effects of Neurokinin-1 Receptor Antagonists
Published in Neuropsychopharmacology (New York, N.Y.) (01-07-2008)“…Several studies have suggested that neurokinin-1 (NK1) receptor antagonists may have therapeutic potential as novel antidepressant drugs. To test these…”
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JD-5006 and JD-5037: Peripherally restricted (PR) cannabinoid-1 receptor blockers related to SLV-319 (Ibipinabant) as metabolic disorder therapeutics devoid of CNS liabilities
Published in Bioorganic & medicinal chemistry letters (01-10-2012)“…Analogs of SLV-319 (Ibipinibant), a CB1 receptor inverse agonist, were synthesized with functionality intended to limit brain exposure while maintaining the…”
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Anxiolytic-like effects of the corticotropin-releasing factor1 (CRF1) antagonist DMP904 [4-(3-pentylamino)-2,7-dimethyl-8-(2-methyl-4-methoxyphenyl)-pyrazolo-[1,5-a]-pyrimidine] administered acutely or chronically at doses occupying central CRF1 receptors in rats
Published in The Journal of pharmacology and experimental therapeutics (01-04-2004)“…Corticotropin-releasing factor(1) (CRF(1)) antagonists may be effective in the treatment of anxiety disorders with fewer side effects compared with classic…”
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Synthesis and Structure−Activity Relationships of 8-(Pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: Potent, Orally Bioavailable Corticotropin Releasing Factor Receptor-1 (CRF1) Antagonists
Published in Journal of medicinal chemistry (14-05-2009)“…This report describes the syntheses and structure−activity relationships of 8-(substituted pyridyl)pyrazolo[1,5-a]-1,3,5-triazine corticotropin releasing…”
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The CRF1 receptor antagonist DMP696 produces anxiolytic effects and inhibits the stress-induced hypothalamic-pituitary-adrenal axis activation without sedation or ataxia in rats
Published in Psychopharmacologia (01-12-2002)“…Abstract Rationale. CRF1 antagonists may be effective in the treatment of anxiety disorders while having fewer side effects compared with classical…”
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Effects of CRF1 receptor antagonists and benzodiazepines in the Morris water maze and delayed non-matching to position tests
Published in Psychopharmacologia (01-04-2005)“…Benzodiazepines continue to be widely used for the treatment of anxiety, but it is well known that benzodiazepines have undesirable side effects, including…”
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The anxiolytic CRF1 antagonist DMP696 fails to function as a discriminative stimulus and does not substitute for chlordiazepoxide in rats
Published in Psychopharmacologia (01-04-2003)“…Rationale. Compounds with a mechanism of action different from benzodiazepines may retain the anxiolytic effects of benzodiazepines with fewer side effects…”
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Novel, highly potent, selective 5-HT2A/D2 receptor antagonists as potential atypical antipsychotics
Published in Bioorganic & medicinal chemistry letters (24-02-2003)“…The discovery of N-substituted-pyridoindolines and their binding affinities at the 5-HT(2A), 5-HT(2C) and D(2) receptors, and in vivo efficacy as 5-HT(2A)…”
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Adverse Effects of Gabapentin and Lack of Anti-Allodynic Efficacy of Amitriptyline in the Streptozotocin Model of Painful Diabetic Neuropathy
Published in Experimental and clinical psychopharmacology (01-02-2006)“…Amitriptyline and gabapentin are the primary treatments for painful diabetic neuropathy (PDN), and it is clear that they produce beneficial effects, but there…”
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Synthesis, Structure−Activity Relationships, and in Vivo Properties of 3,4-Dihydro-1H-pyrido[2,3-b]pyrazin-2-ones as Corticotropin-Releasing Factor-1 Receptor Antagonists
Published in Journal of medicinal chemistry (04-11-2004)“…Corticotropin releasing factor (CRF) is the primary regulator of the hypothalamus−pituitary−adrenal (HPA) axis, coordinating the endocrine, behavioral, and…”
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Novel piperidine .sigma. receptor ligands as potential antipsychotic drugs
Published in Journal of medicinal chemistry (01-11-1992)“…sigma receptor ligands represent a new class of potential antipsychotic drugs. This paper presents the structure-activity relationships leading to novel…”
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Short- and long-term effects of ovariectomy on food intake, body weight, carcass composition, and brown adipose tissue in rats
Published in Physiology & behavior (1987)“…This experiment examined both the short-term and the long-term effects of ovariectomy on brown adipose tissue growth and function in rats to determine if…”
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Piperidinyltetralin .sigma. Ligands
Published in Journal of medicinal chemistry (01-02-1994)“…Sigma receptor ligands have been proposed to be potential antipsychotic drugs based on their activity profile in animal behavioral models and their indirect…”
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Repetition, Contrariety, and Individualization in Edward II
Published in Studies in English literature, 1500-1900 (01-04-1984)Get full text
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Effects of CRF sub(1) receptor antagonists and benzodiazepines in the Morris water maze and delayed non-matching to position tests
Published in Psychopharmacology (01-04-2005)“…Rationale: Benzodiazepines continue to be widely used for the treatment of anxiety, but it is well known that benzodiazepines have undesirable side effects,…”
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The anxiolytic CRF(1) antagonist DMP696 fails to function as a discriminative stimulus and does not substitute for chlordiazepoxide in rats
Published in Psychopharmacology (01-04-2003)“…Compounds with a mechanism of action different from benzodiazepines may retain the anxiolytic effects of benzodiazepines with fewer side effects. CRF(1)…”
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The CRF(1) receptor antagonist DMP696 produces anxiolytic effects and inhibits the stress-induced hypothalamic-pituitary-adrenal axis activation without sedation or ataxia in rats
Published in Psychopharmacology (01-12-2002)“…CRF(1) antagonists may be effective in the treatment of anxiety disorders while having fewer side effects compared with classical benzodiazepines. The effects…”
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