3-[2-Cyano-3-(trifluoromethyl)phenoxy]phenyl-4,4,4-trifluoro-1-butanesulfonate (BAY 59-3074): A Novel Cannabinoid CB1/CB2 Receptor Partial Agonist with Antihyperalgesic and Antiallodynic Effects
@article{Vry200432Cyano3trifluoromethylphenoxyphenyl44, title={3-[2-Cyano-3-(trifluoromethyl)phenoxy]phenyl-4,4,4-trifluoro-1-butanesulfonate (BAY 59-3074): A Novel Cannabinoid CB1/CB2 Receptor Partial Agonist with Antihyperalgesic and Antiallodynic Effects}, author={J. de Vry and D. Denzer and E. Reissmueller and Maud Eijckenboom and M. Heil and H. Meier and F. Mauler}, journal={Journal of Pharmacology and Experimental Therapeutics}, year={2004}, volume={310}, pages={620 - 632} }
3-[2-Cyano-3-(trifluoromethyl)phenoxy]phenyl-4,4,4-trifluoro-1-butanesulfonate (BAY 59-3074) is a novel, selective cannabinoid CB1/CB2 receptor ligand (Ki = 55.4, 48.3, and 45.5 nM at rat and human cannabinoid CB1 and human CB2 receptors, respectively), with partial agonist properties at these receptors in guanosine 5-[γ35S]-thiophosphate triethyl-ammonium salt ([35S]GTPγS) binding assays. In rats, generalization of BAY 59-3074 to the cue induced by the cannabinoid CB1 receptor agonist (–)-(R… CONTINUE READING
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References
SHOWING 1-10 OF 46 REFERENCES
Characterization of the diarylether sulfonylester (-)-(R)-3-(2-hydroxymethylindanyl-4-oxy)phenyl-4,4,4-trifluoro-1-sulfonate (BAY 38-7271) as a potent cannabinoid receptor agonist with neuroprotective properties.
- Chemistry, Medicine
- The Journal of pharmacology and experimental therapeutics
- 2002
- 95
- PDF
delta 9-Tetrahydrocannabinol is a partial agonist of cannabinoid receptors in mouse brain.
- Biology, Medicine
- European journal of pharmacology
- 1997
- 55
Discriminative stimulus effects of BAY 38-7271, a novel cannabinoid receptor agonist.
- Medicine
- European journal of pharmacology
- 2002
- 12
Large receptor reserve for cannabinoid actions in the central nervous system.
- Biology, Medicine
- The Journal of pharmacology and experimental therapeutics
- 1999
- 107
- PDF
Behavioral, biochemical, and molecular modeling evaluations of cannabinoid analogs
- Chemistry, Medicine
- Pharmacology Biochemistry and Behavior
- 1991
- 368
Intrinsic activity estimation of cannabinoid CB1 receptor ligands in a drug discrimination paradigm
- Chemistry, Medicine
- Behavioural pharmacology
- 2003
- 29
Nociceptin and the ORL‐1 ligand [Phe1ψ (CH2‐NH)Gly2]nociceptin(1‐13)NH2 exert anti‐opioid effects in the Freund's adjuvant‐induced arthritic rat model of chronic pain
- Medicine
- British journal of pharmacology
- 1999
- 58
The analgesic effects of R(+)-WIN 55,212–2 mesylate, a high affinity cannabinoid agonist, in a rat model of neuropathic pain
- Medicine
- Neuroscience Letters
- 1997
- 286
Discriminative stimulus effects of CP 55,940 and structurally dissimilar cannabinoids in rats
- Chemistry, Medicine
- Neuropharmacology
- 1995
- 122