Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 7 of 7 for “"CB1-antagonist"”.
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Discriminative stimulus properties of 3-substituent rimonabant analogs
… a limited dose range are likely to function as CB1 receptor agonists. A structure activity relationship study from our laboratory investigating analogs of the CB1 antagonist rimonabant revealed that certain alterations in the 3-substituent of rimonabant’s pyrazole core conferred agonist-like …
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Cannabinoid Modulation of Reinforcement Maintained by Stimulation of the Medial Forebrain Bundle in C57Bl/6J Mice
… reductions in ICSS that were mediated through CB1 receptors, as they were blocked by pre-treatment with the CB1 antagonist rimonabant, but not with the CB2 antagonist SR144528. PF-3845 also reduced ICSS, but did so independent of CB1 and CB2 receptors, and only with one dose (30.0 mg/kg) that …
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Novel Insights into CB1 Receptor Signaling and the Anabolic Role of Cannabinoid Receptors in Bone
Activation of the CB1 receptor is modulated by aspartate residue D2.63176 in transmembrane helix (TMH) II. Interestingly, D2.63 does not affect the affinity for ligand binding at the CB1 receptor. Studies in class A GPCRs have suggested an ionic interaction between residues of TMHII and VII. In …
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Characterization of Rimonabant effects on G protein activity
… inverse agonists (Milligan, 2003). Cannabinoid CB1 receptor is one of the most abundant GPCR in the central nervous system, and is coupled to Gi/o proteins to inhibit adenylyl cyclase, activate mitogen-activated protein kinase (MAPK), inhibit voltage gated Ca2+ channels and activate inwardly …
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Caratterizzazione del clofibrato agonista sintetico dei recettori dei proliferatori dei perossisomi (PPARα)in modelli animali di depressione ed ansia
… Acute administration of the specific PPARα antagonist MK886 (1 mg/kg, i.p) or the CB1 antagonist/inverse agonist SR141716A (1 mg/kg, i.p) did no antagonize the antidepressant-like effect induced by classical antidepressant drugs. In contrast the antidepressant-like affects of clofibrate were …
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Studies on transient receptor potential vanilloid subtype 1 (TRPV1)-mediated degeneration of mesencephalic cellsin vivo and in vitro
… and in vitro effect was ameliorated by the TRPV1 antagonist capsazepine (CZP) or iodo-resiniferatoxin (I-RTX), suggesting the direct involvement of TRPV1 in neurotoxicity. In cultures, both CAP and anandamide (AEA), an endogenous ligand for both TRPV1 and cannabinoid type 1 (CB1) receptors, …
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Design, Synthesis and Biological Evaluation of Novel Cannabinoid Antagonist
… study was aimed at the development of novel CB1 cannabinoid receptor antagonists that may have clinical applications for the treatment of cannabinoid and psychostimulant addiction. The rationale for the design for our target was to incorporate a bioisosteric 1,2,3-triazole ring into the …