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In vivo characterization of a specific cannabinoid receptor antagonist (SR141716A): inhibition of delta 9-tetrahydrocannabinol-induced responses and apparent agonist activity.
TLDR
It is not clear whether this pharmacological activity represents an uncharacterized action of SR141716A, or an index of tonic activity of an endogenous cannabinergic system, but it will be useful in establishing the biochemical events responsible for the in vivo effects of exogenous cannabinoids, as well as inestablishing the existence of a putative endogenous cannabinoidergic system. Expand
Ziprasidone (CP-88,059): a new antipsychotic with combined dopamine and serotonin receptor antagonist activity.
TLDR
The prediction of antipsychotic efficacy without severe motor side effects is supported by the relatively weak potency of ziprasidone to produce catalepsy in animals, contrasted with its potent antagonism of conditioned avoidance responding and dopamine agonist-induced locomotor activation and stereotypy. Expand
A potent nonpeptide antagonist of the substance P (NK1) receptor.
TLDR
CP-96,345 inhibited substance P-induced salivation in the rat, a classical in vivo bioassay, but did not inhibit NK2, NK3, or numerous other receptors; it is thus a selective NK1 antagonist. Expand
Antagonism of the discriminative stimulus effects of delta 9-tetrahydrocannabinol in rats and rhesus monkeys.
TLDR
The present results suggest that SR141716A blocks the discriminative stimulus effects of delta 9-THC via a receptor-mediated mechanism and is predicted to block or reverse cannabis intoxication in humans. Expand
Partial Agonists of the α3β4* Neuronal Nicotinic Acetylcholine Receptor Reduce Ethanol Consumption and Seeking in Rats
TLDR
It is shown that the functional potencies of CP-601932 and PF-4575180 at α3β4 nAChRs correlate with their unbound rat brain concentrations, suggesting that the effects on ethanol self-administration are mediated via interaction with α3 β4 n AChRs. Expand
Effects of the cannabinoid CB1 receptor antagonist SR141716A on the behavior of pigeons and rats
TLDR
Results suggest that SR is an effective antagonist of the psychoactive effects of cannabinoids, as evaluated in acoustic startle procedures in rats. Expand
Glycine transporter type 1 blockade changes NMDA receptor‐mediated responses and LTP in hippocampal CA1 pyramidal cells by altering extracellular glycine levels
TLDR
The data suggest that the level of glycine present in the synaptic cleft tightly regulates the NMDAR activity, kept below the ‘set point’ of the N MDAR internalization priming mechanism by the presence of GlyT1‐dependent uptake. Expand
Discriminative stimulus effects of CP 55,940 and structurally dissimilar cannabinoids in rats
TLDR
It is demonstrated that CP 55,940 has discriminative stimulus effects and that it shares these effects with structurally dissimilar compounds that, like CP55,940, bind to the cannabinoid receptor. Expand
Differential blockade of the antinociceptive effects of centrally administered cannabinoids by SR141716A.
TLDR
Data indicate that SR has a much greater efficacy at supraspinal than at spinal sites and suggest either a differential interaction of the cannabinoids at the CB1 receptor or the existence of subtypes of the cannabinoid (CB1) receptor. Expand
Characterization of Δ9-Tetrahydrocannabinol and Anandamide Antinociception in Nonarthritic and Arthritic Rats
TLDR
It is indicated that anandamide and THC may act at different receptor sites to modulate endogenous opioid levels in mechanical nociception. Expand
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