JWH-051
Encyclopedia
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 Dr. 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.
Analgesic
An analgesic is any member of the group of drugs used to relieve pain . The word analgesic derives from Greek an- and algos ....
drug which is a cannabinoid agonist
Agonist
An agonist is a chemical that binds to a receptor of a cell and triggers a response by that cell. Agonists often mimic the action of a naturally occurring substance...
. Its chemical structure is closely related to that of the potent cannabinoid agonist HU-210
HU-210
HU-210 is a synthetic cannabinoid that was first synthesized in 1988 from -Myrtenol by the group led by Professor Raphael Mechoulam at the Hebrew University. HU-210 is 100 to 800 times more potent than natural THC from cannabis and has an extended duration of action...
, with the only difference being the removal of the hydroxyl group at position 1 of the aromatic ring. It was discovered and named after Dr. John W. Huffman
John W. Huffman
John William Huffman is a professor emeritus of organic chemistry at Clemson University who first synthesised many novel cannabinoids, including JWH-007, JWH-015, JWH-018, JWH-019, JWH-030, JWH-051, JWH-073, JWH-081, JWH-122, JWH-133, JWH-147, JWH-171, JWH-182, JWH-203, JWH-210, JWH-250, JWH-307,...
.
JWH-051 retains high affinity for the CB1 receptor
Receptor (biochemistry)
In biochemistry, a receptor is a molecule found on the surface of a cell, which receives specific chemical signals from neighbouring cells or the wider environment within an organism...
, but is a much stronger agonist for CB2, with a Ki
Dissociation constant
In chemistry, biochemistry, and pharmacology, a dissociation constant is a specific type of equilibrium constant that measures the propensity of a larger object to separate reversibly into smaller components, as when a complex falls apart into its component molecules, or when a salt splits up into...
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
HU-308
HU-308 is a drug which acts as a cannabinoid agonist. It is highly selective for the CB2 receptor subtype, with a selectivity of over 5000x for CB2 vs CB1. The synthesis and characterization took place in the laboratory of Prof. Mechoulam at the Hebrew University of Jerusalem in the late 1990s...
.
It has similar effects to other cannabinoid agonists such as sedation
Sedation
Sedation is the reduction of irritability or agitation by administration of sedative drugs, generally to facilitate a medical procedure or diagnostic procedure...
and analgesia, but with a relatively strong antiinflammatory effect due to its strong activity at CB2.