cep-26401 and Disease-Models--Animal

cep-26401 has been researched along with Disease-Models--Animal* in 2 studies

Other Studies

2 other study(ies) available for cep-26401 and Disease-Models--Animal

Article	Year
Discovery of (1R,6S)-5-[4-(1-cyclobutyl-piperidin-4-yloxy)-phenyl]-3,4-diaza-bicyclo[4.1.0]hept-4-en-2-one (R,S-4a): histamine H(3) receptor inverse agonist demonstrating potent cognitive enhancing and wake promoting activity. Bioorganic & medicinal chemistry letters, 2014, Mar-01, Volume: 24, Issue:5 A series of fused cyclopropyl-4,5-dihydropyridazin-3-one (3,4-diaza-bicyclo[4.1.0]hept-4-en-2-one) phenoxypiperidine analogs was designed and synthesized, leading to the identification of (1R,6S)-5-[4-(1-cyclobutyl-piperidin-4-yloxy)-phenyl]-3,4-diaza-bicyclo[4.1.0]hept-4-en-2-one (R,S-4a) as a second-generation pyridazin-3-one H3R antagonist. Compound R,S-4a was a potent H3R functional antagonist in vivo in the rat dipsogenia model, demonstrated potent wake activity in the rat EEG/EMG model, and enhanced short-term memory in the rat social recognition memory model at doses as low as 0.03-0.3 mg/kg po. Topics: Animals; Cognition Disorders; Disease Models, Animal; Dogs; Drug Evaluation, Preclinical; Drug Inverse Agonism; Half-Life; Haplorhini; Memory, Short-Term; Nootropic Agents; Piperidines; Pyridazines; Rats; Receptors, Histamine H3; Stereoisomerism; Structure-Activity Relationship	2014
Identification of pyridazin-3-one derivatives as potent, selective histamine H₃ receptor inverse agonists with robust wake activity. Bioorganic & medicinal chemistry letters, 2011, Sep-15, Volume: 21, Issue:18 H(3)R structure-activity relationships on a novel class of pyridazin-3-one H(3)R antagonists/inverse agonists are disclosed. Modifications of the pyridazinone core, central phenyl ring and linker led to the identification of molecules with excellent target potency, selectivity and pharmacokinetic properties. Compounds 13 and 21 displayed potent functional H(3)R antagonism in vivo in the rat dipsogenia model and demonstrated robust wake activity in the rat EEG/EMG model. Topics: Animals; Disease Models, Animal; Dose-Response Relationship, Drug; Drinking; Histamine Agonists; Humans; Male; Molecular Structure; Pyridazines; Rats; Receptors, Histamine H3; Stereoisomerism; Structure-Activity Relationship; Wakefulness	2011

Article

Year

Discovery of (1R,6S)-5-[4-(1-cyclobutyl-piperidin-4-yloxy)-phenyl]-3,4-diaza-bicyclo[4.1.0]hept-4-en-2-one (R,S-4a): histamine H(3) receptor inverse agonist demonstrating potent cognitive enhancing and wake promoting activity.

Bioorganic & medicinal chemistry letters, 2014, Mar-01, Volume: 24, Issue:5

A series of fused cyclopropyl-4,5-dihydropyridazin-3-one (3,4-diaza-bicyclo[4.1.0]hept-4-en-2-one) phenoxypiperidine analogs was designed and synthesized, leading to the identification of (1R,6S)-5-[4-(1-cyclobutyl-piperidin-4-yloxy)-phenyl]-3,4-diaza-bicyclo[4.1.0]hept-4-en-2-one (R,S-4a) as a second-generation pyridazin-3-one H3R antagonist. Compound R,S-4a was a potent H3R functional antagonist in vivo in the rat dipsogenia model, demonstrated potent wake activity in the rat EEG/EMG model, and enhanced short-term memory in the rat social recognition memory model at doses as low as 0.03-0.3 mg/kg po.

Topics: Animals; Cognition Disorders; Disease Models, Animal; Dogs; Drug Evaluation, Preclinical; Drug Inverse Agonism; Half-Life; Haplorhini; Memory, Short-Term; Nootropic Agents; Piperidines; Pyridazines; Rats; Receptors, Histamine H3; Stereoisomerism; Structure-Activity Relationship

2014

Identification of pyridazin-3-one derivatives as potent, selective histamine H₃ receptor inverse agonists with robust wake activity.

Bioorganic & medicinal chemistry letters, 2011, Sep-15, Volume: 21, Issue:18

H(3)R structure-activity relationships on a novel class of pyridazin-3-one H(3)R antagonists/inverse agonists are disclosed. Modifications of the pyridazinone core, central phenyl ring and linker led to the identification of molecules with excellent target potency, selectivity and pharmacokinetic properties. Compounds 13 and 21 displayed potent functional H(3)R antagonism in vivo in the rat dipsogenia model and demonstrated robust wake activity in the rat EEG/EMG model.

Topics: Animals; Disease Models, Animal; Dose-Response Relationship, Drug; Drinking; Histamine Agonists; Humans; Male; Molecular Structure; Pyridazines; Rats; Receptors, Histamine H3; Stereoisomerism; Structure-Activity Relationship; Wakefulness

2011