Design and synthesis of the CB1 selective cannabinoid antagonist AM281: A potential human SPECT ligand
نویسندگان
چکیده
منابع مشابه
AM281, Cannabinoid Antagonist/Inverse agonist, Ameliorates Scopolamine-Induced Cognitive Deficit
Objective(s) Cannabinoids have been implicated in memory deficit. We examined the effect of AM281, cannabinoid antagonist/inverse agonist in prevention of scopolamine-induced cognitive deficit. Materials and Methods Object recognition task was used to evaluate memory in mice. Exploration time in the first and the second trial was recorded. The differences in exploration between a previously...
متن کاملAM281, Cannabinoid Antagonist/Inverse agonist, Ameliorates Scopolamine-Induced Cognitive Deficit
OBJECTIVES Cannabinoids have been implicated in memory deficit. We examined the effect of AM281, cannabinoid antagonist/inverse agonist in prevention of scopolamine-induced cognitive deficit. MATERIALS AND METHODS Object recognition task was used to evaluate memory in mice. Exploration time in the first and the second trial was recorded. The differences in exploration between a previously see...
متن کاملSynthesis and characterization of NESS 0327: a novel putative antagonist of the CB1 cannabinoid receptor.
The compound N-piperidinyl-[8-chloro-1-(2,4-dichlorophenyl)-1,4,5,6-tetrahydrobenzo [6,7]cyclohepta[1,2-c]pyrazole-3-carboxamide] (NESS 0327) was synthesized and evaluated for binding affinity toward cannabinoid CB1 and CB2 receptor. NESS 0327 exhibited a stronger selectivity for CB1 receptor compared with N-piperidinyl-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamid...
متن کاملam281, cannabinoid antagonist/inverse agonist, ameliorates scopolamine-induced cognitive deficit
objective(s) cannabinoids have been implicated in memory deficit. we examined the effect of am281, cannabinoid antagonist/inverse agonist in prevention of scopolamine-induced cognitive deficit. materials and methods object recognition task was used to evaluate memory in mice. exploration time in the first and the second trial was recorded. the differences in exploration between a previously se...
متن کاملRimonabant, a selective cannabinoid CB1 receptor antagonist, inhibits atherosclerosis in LDL receptor-deficient mice.
OBJECTIVE The objective of this study was to determine whether the potent selective cannabinoid receptor-1 antagonist rimonabant has antiatherosclerotic properties. METHODS AND RESULTS Rimonabant (50 mg/kg/d in the diet) significantly reduced food intake (from 3.35+/-.04 to 2.80+/-0.03 g/d), weight gain (from 14.6+/-0.7 g to -0.6+/-0.3 g), serum total cholesterol (from 8.39+/-0.54 to 5.32+/-0...
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ژورنال
عنوان ژورنال: AAPS PharmSci
سال: 1999
ISSN: 1522-1059
DOI: 10.1208/ps010204