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Cannabinoid agonists and antagonists

III. Effects of Exogenously Administered Cannabinoid Agonists and Antagonists... [Pg.57]

Thomas BF, Gilliam AF, Burch DF, Roche MJ, Seltzman HH (1998) Comparative receptor binding analyses of cannabinoid agonists and antagonists. J Pharmacol Exp Ther 285 285-292... [Pg.246]

Parker LA, Mechoulam R (2003) Cannabinoid agonists and antagonists modulate lithium-induced conditioned gaping in rats. Integr Physiol Behav Sci 38 134-146... [Pg.596]

Cannabinoid agonists and antagonists that are not stmc-turally related to THC have been synthesised for diverse therapeutic indications. One of them is Rimonabant ... [Pg.287]

Figure 14.20 Non-structurally related cannabinoid agonist and antagonist. Figure 14.20 Non-structurally related cannabinoid agonist and antagonist.
Tables 6.8-6.11 illustrate the wide range of C3 side-chain modified A -THC analogues that have been reported in the literature, together with associated in vitro and in vivo data. The affinity of classical cannabinoid analogues for the CBi receptor has been shown to correlate with depression of spontaneous activity and the production of antinociception, hypothermia and catalepsy in mice, and with psychomimetic activity in humans [93]. However, in some cases, there were unexplained differences between the observed trends in binding affinity and the trends in activity in mouse behavioural models. This may point to differences in efficacy among full agonists, partial agonists and antagonists/inverse agonists, or may reflect differences in in vivo metabolism or blood-brain barrier penetration or a combination of these factors. Tables 6.8-6.11 illustrate the wide range of C3 side-chain modified A -THC analogues that have been reported in the literature, together with associated in vitro and in vivo data. The affinity of classical cannabinoid analogues for the CBi receptor has been shown to correlate with depression of spontaneous activity and the production of antinociception, hypothermia and catalepsy in mice, and with psychomimetic activity in humans [93]. However, in some cases, there were unexplained differences between the observed trends in binding affinity and the trends in activity in mouse behavioural models. This may point to differences in efficacy among full agonists, partial agonists and antagonists/inverse agonists, or may reflect differences in in vivo metabolism or blood-brain barrier penetration or a combination of these factors.
Mouse vas deferens (MVD) seems to express CB1 and at least one CB2-like cannabinoid receptor type, as is demonstrated by the presence of CB1 and CB2-like mRNA as well as by data collected from experiments with cannabinoid receptor selective agonists and antagonists (Pertwee, 1999). Furthermore, evidence indicates that a CBl-like receptor exists in vascular endothelium, which upon activation produces significant hypotension (Wagner, 1999). This receptor differs from CB1 in its pharmacological response to some well-characterized cannabimimetics. [Pg.99]

Keywords Cannabinoid receptors Cannabinoid receptor agonists and antagonists Abnormal-cannabidiol Cannabidiol Inverse agonism... [Pg.2]

Griffin GR, Atkinson PJ, Showalter VM, Martin BR, Abood ME (1998) Evaluation of cannabinoid receptor agonists and antagonists using the guanosine-5 -O-(3-[35S]thio)-triphosphate binding assay in rat cerebellar membranes. J Pharmacol Exp Ther 285 553-560... [Pg.109]

Smith SR, Terminelli C, Denhardt G (2000) Effects of cannabinoid receptor agonist and antagonist ligands on production of inflammatory cytokines and anti-inflammatory interleukin-10 in endotoxemic mice. J Pharmacol Exp Ther 293 136-150... [Pg.422]

Meschler JP, Howlett AC, Madras BK (2001) Cannabinoid receptor agonist and antagonist effects on motor function in normal and l-methyl-4-phenyl-l,2,5,6-tetrahydropyridine (MPTP)-treated non-human primates. Psychopharmacology (Berl) 156 79-85... [Pg.504]

Likewise, systemically administered cannabinoid CBj ligands (both agonists and antagonists) appear to affect food intake and appetite predominantly by engaging peripheral CBj receptors... [Pg.410]

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Agonists and Antagonists

Cannabinoid

Cannabinoid antagonists

Cannabinoids

Cannabinoids, antagonists

Effects of Exogenously Administered Cannabinoid Agonists and Antagonists

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