• Publications
  • Influence
Cannabinoid receptor localization in brain.
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.
The criteria for a high affinity, stereoselective, pharmacologically distinct cannabinoid receptor in brain tissue have been fulfilled.
Cannabinoid structure-activity relationships: correlation of receptor binding and in vivo activities.
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.
Pharmacology and stereoselectivity of structurally novel cannabinoids in mice.
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.
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.
Pharmacological profile of a series of bicyclic cannabinoid analogs: classification as cannabimimetic agents.
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.
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.
Cannabinoid receptor binding and agonist activity of amides and esters of arachidonic acid.
It appears that the bulk and length of the moiety appended to arachidonic acid are more important determinants of affinity for CB1 than is hydrogen-bonding capability.
Structure-activity relationships for cannabinoid receptor-binding and analgesic activity: studies of bicyclic cannabinoid analogs.
Several series of CP-47,497 analogs are examined for their binding affinity at the cannabinoid receptor and their ability to evoke analgesia in rodents and in general, analgesic activity correlated well with the affinity of these analogs for the cannabinoids receptor.
The discovery of a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase--GW311616A a development candidate.
The discovery of a potent intracellular inhibitor of human neutrophil elastase which is orally active and has a long duration of action is described. The pharmacodynamic and pharmacokinetic