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Cannabinoid receptor localization in brain.
TLDR
The potencies of a series of natural and synthetic cannabinoids as competitors of [3H]CP 55,940 binding correlated closely with their relative potencies in several biological assays, suggesting that the receptor characterized in the in vitro assay is the same receptor that mediates behavioral and pharmacological effects of cannabinoids, including human subjective experience.
Determination and characterization of a cannabinoid receptor in rat brain.
TLDR
The criteria for a high affinity, stereoselective, pharmacologically distinct cannabinoid receptor in brain tissue have been fulfilled.
Behavioral, biochemical, and molecular modeling evaluations of cannabinoid analogs
TLDR
The structural diversity and wide-ranging potencies of the analogs described herein provide the opportunity to develop a pharmacophore for the cannabinoids using molecular modeling techniques.
Cannabinoid structure-activity relationships: correlation of receptor binding and in vivo activities.
TLDR
High correlations were demonstrated between binding affinity and in vivo potency in both the rat drug discrimination model and for psychotomimetic activity in humans, and the structure-activity relationship indicated the importance of side chain structure to high-affinity binding.
Development of cross-tolerance between delta 9-tetrahydrocannabinol, CP 55,940 and WIN 55,212.
TLDR
Findings indicate that cross-tolerance develops between delta 9-THC, CP 55,940 and WIN 55,212 and that these agents have some actions in common, however, quantitative differences in their development of cross-Tolerance suggests that all of their actions may not be identical.
Pharmacology and stereoselectivity of structurally novel cannabinoids in mice.
TLDR
The pharmacological effects of three stereoisomeric pairs of structurally novel cannabinoids were tested after i.v. administration in mice for depression of spontaneous activity and the production of hypothermia, antinociception and catalepsy to demonstrate the high degree of enantioselectivity and potency.
Nonclassical cannabinoid analgetics inhibit adenylate cyclase: development of a cannabinoid receptor model.
TLDR
It is postulated that the receptor that is associated with the regulation of adenylate cyclase in vitro may be the same receptor as that mediating analgesia in vivo, and a conceptualization of the cannabinoid analgetic receptor is presented.
The cannabinoid receptor: biochemical, anatomical and behavioral characterization
TLDR
The actions of the active principle of marihuana, delta 9-tetrahydrocannabinol, are mimicked by synthetic cannabinoid agonists showing high potency and enantio-selectivity in behavioral assays, leading to a better understanding of the effects of cannabinoids in the CNS of humans and experimental animals.
Pharmacological profile of a series of bicyclic cannabinoid analogs: classification as cannabimimetic agents.
TLDR
The goals of the studies described herein were to determine whether these bicyclic analogs possess similar pharmacological properties of delta 9-THC, to compare pharmacological activity after s.c. and i.v. administration, and to evaluate the structure-activity relationship of this series of analogs for further insight into cannabinoid mechanism of action.
A cannabinoid derived prototypical analgesic.
TLDR
Biological testing in five models of pain shows that compound 1 and morphine are equally potent as analgesics and demonstrates that the pyran ring of HHC is not necessary for biological activity.
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