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-
tetramethylcyclopropyl
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 CB
2, and A-796,260 was found to be a highly selective CB
2 agonist with little affinity for CB
1, having a CB
2 ''K''i of 4.6 nM vs 945 nM at CB
1. 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.
See also
*
A-834,735
*
A-836,339
*
BMS-F
*
JWH-200
*
UR-144
UR-144 (TMCP-018, KM-X1, MN-001, YX-17) is a drug invented by Abbott Laboratories, that acts as a selective full agonist of the peripheral cannabinoid receptor CB2, but with much lower affinity for the psychoactive CB1 receptor.
Pharmacology
U ...
*
XLR-11
XLR-11 (5"-fluoro-UR-144 or 5F-UR-144) is a drug that acts as a potent agonist for the cannabinoid receptors CB1 and CB2 with EC50 values of 98 nM and 83 nM, respectively. It is a 3-(tetramethylcyclopropylmethanoyl)indole derivative related t ...
References
Cannabinoids
Cyclopropanes
Aminoalkylindoles
Tetramethylcyclopropanoylindoles
{{cannabinoid-stub