A-796,260 is a drug developed by

Abbott Laboratories Abbott Laboratories is an American multinational medical devices and health care company with headquarters in Abbott Park, Illinois, in the United States. The company was founded by Chicago physician Wallace Calvin Abbott in 1888 to formulate k ...

that acts as a potent and selective

cannabinoid Cannabinoids () are several structural classes of compounds found primarily in the ''Cannabis'' plant or as synthetic compounds. The most notable cannabinoid is the phytocannabinoid tetrahydrocannabinol (THC) (delta-9-THC), the primary psychoact ...

CB₂

receptor Receptor may refer to: * Sensory receptor, in physiology, any neurite structure that, on receiving environmental stimuli, produces an informative nerve impulse *Receptor (biochemistry), in biochemistry, a protein molecule that receives and respond ...

agonist An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an R ...

. Replacing the aromatic 3- benzoyl or 3-

naphthoyl Naphthoyl (naphthalenecarbonyl) is an acyl group derived from naphthoic acid. It may refer to: * 1-naphthoyl (naphthalene-1-carbonyl), derived from 1-naphthoic acid * 2-naphthoyl (naphthalene-2-carbonyl), derived from 2-naphthoic acid See als ...

group found in most

indole Indole is an organic compound with the formula . Indole is classified as an aromatic heterocycle. It has a bicyclic structure, consisting of a six-membered benzene ring fused to a five-membered pyrrole ring. Indoles are derivatives of indole ...

derived cannabinoids with the 3- tetramethyl

cyclopropyl A cyclopropyl group is a chemical structure derived from cyclopropane; it is typically produced in a cyclopropanation reaction. The group has an empirical formula of C3H5 and chemical bonds from each of the three carbons to both of the other tw ...

methanone group, imparts significant selectivity for CB₂, and A-796,260 was found to be a highly selective CB₂ agonist with little affinity for CB₁, having a CB₂ ''K''_i of 4.6 nM vs 945 nM at CB₁. It has potent

analgesic An analgesic drug, also called simply an analgesic, antalgic, pain reliever, or painkiller, is any member of the group of drugs used for pain management. Analgesics are conceptually distinct from anesthetics, which temporarily reduce, and in s ...

and

anti-inflammatory Anti-inflammatory is the property of a substance or treatment that reduces inflammation, fever or swelling. Anti-inflammatory drugs, also called anti-inflammatories, make up about half of analgesics. These drugs reduce pain by inhibiting mechan ...

actions in animal models, being especially effective in models of

neuropathic pain Neuropathic pain is pain caused by a lesion or disease of the somatosensory nervous system. Neuropathic pain may be associated with abnormal sensations called dysesthesia or pain from normally non-painful stimuli (allodynia). It may have continuo ...

, but without producing cannabis-like behavioral effects.

Legal Status

As of October 2015 A-796,260 is a controlled substance in China.

References

Cannabinoids Cyclopropanes Aminoalkylindoles Tetramethylcyclopropanoylindoles {{cannabinoid-stub

Legal Status

See also

References