| Name | Bay 59-3074 |
| Description | Bay 59-3074 is a CB1/CB2 receptor partial agonist (Ki: 48.3/45.5 nM). In rat models of chronic neuropathic and inflammatory pain, it displays anti-hyperalgesic and antiallodynic properties. |
| In vitro | analgesic, antihyperalgesic, and antiallodynic properties in rat models of acute and chronic pain. The reference concentration is 10 μM. |
| In vivo | In rat models of chronic neuropathic (chronic constriction injury, spared nerve injury, tibial nerve injury, and spinal nerve ligation models) and inflammatory pain (carrageenan and complete Freund's adjuvant models), BAY 59-3074 (0.3-3 mg/kg, p.o.) induced antihyperalgesic and antiallodynic effects against thermal or mechanical stimuli. Antiallodynic efficacy of BAY 59-3074 (1 mg/kg, p.o.) in the spared nerve injury model was maintained after 2 weeks of daily administration. However, tolerance developed rapidly (within 5 days) for cannabinoid-related side effects, which occur at doses above 1 mg/kg (e.g., hypothermia). Uptitration from 1 to 32 mg/kg p.o. (doubling of daily dose every 4th day) prevented the occurrence of such side effects, whereas antihyperalgesic and antiallodynic efficacy was maintained/increased. No withdrawal symptoms were seen after abrupt withdrawal following 14 daily applications of 1 to 10 mg/kg p.o. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+90% Corn Oil : 2.5 mg/mL (5.51 mM), Sonication is recommended.
DMSO : 50 mg/mL (110.29 mM), Sonication is recommended.
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| Keywords | Inhibitor | inhibit | CB2 | CB1 | CB | CannabinoidReceptor | Cannabinoid Receptor | Bay 59-3074 | Bay 593074 | Bay 59 3074 |
| Inhibitors Related | RTICBM-189 | β-Caryophyllene | CB2 modulator 1 | Pregnenolone | Pregnenolone acetate | CB1 antagonist 2 | Dehydroabiethylamine | CB2 receptor agonist 2 | AM-1235 | 2,3-Butanediol | Drinabant | AM281 |
| Related Compound Libraries | Bioactive Compound Library | Pain-Related Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | Neurotransmitter Receptor Compound Library | Mitochondria-Targeted Compound Library | NO PAINS Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Covalent Inhibitor Library | GPCR Compound Library | Anti-Cancer Compound Library |
United States
