JWH-051 is an analgesic drug which is a cannabinoid agonist. Its chemical structure is closely related to that of the potent cannabinoid agonist HU-210, with the only difference being the removal of the hydroxyl group at position 1 of the aromatic ring.
It was discovered and named after John W. Huffman.
JWH-051 retains high affinity for the CB1 receptor,
but is a much stronger agonist for CB2, with a Ki value of 14nM at CB2 vs 19nM at CB1.
It was one of the first CB2-selective ligands developed,
although its selectivity for CB2 is modest compared to newer compounds such as HU-308.
JWH-051
JWH-051 is an analgesic drug which is a cannabinoid agonist.
Its chemical structure is closely related to that of the potent cannabinoid agonist HU-210,
with the only difference being the removal of the hydroxyl group at position 1 of the aromatic ring.
It was discovered and named after John W. Huffman.
JWH-051 retains high affinity for the CB1 receptor, but is a much stronger agonist for CB2, with a Ki value of 14nM at CB2 vs 19nM at CB1.
It was one of the first CB2-selective ligands developed, although its selectivity for CB2 is modest compared to newer compounds such as HU-308.
It has similar effects to other cannabinoid agonists such as sedation and analgesia,
but with a relatively strong antiinflammatory effect due to its strong activity at CB2
Cannabinoid Receptor 2 Agonist JWH-015 Inhibits Interleukin-1β-Induced Inflammation in Rheumatoid Arthritis Synovial Fibroblasts and in Adjuvant Induced Arthritis Rat via Glucocorticoid Receptor
Management of pain in the treatment of rheumatoid arthritis (RA) is a priority that is not fully addressed by the conventional therapies.
In the present study, we evaluated the efficacy of cannabinoid receptor 2 (CB2) agonist
JWH-015 using RA synovial fibroblasts (RASFs) obtained from
patients diagnosed with RA and in a rat adjuvant-induced arthritis (AIA) model of RA.
Pretreatment of human RASFs with JWH-015 (10–20 μM) markedly
inhibited the ability of pro-inflammatory cytokine interleukin-1β (IL-1β)
to induce production of IL-6 and IL-8 and
cellular expression of inflammatory cyclooxygenase-2 (COX-2).
JWH-015 was effective in reducing IL-1β-induced phosphorylation of TAK1 (Thr184/187) and
JNK/SAPK in human RASFs. While the knockdown of CB2 in RASFs using siRNA method reduced IL-1β-induced inflammation
