A-796,260
Encyclopedia
A-796,260 is a drug developed by Abbott Laboratories
which acts as a potent and selective cannabinoid CB2 receptor
agonist
. Replacing the aromatic 3-benzoyl
or 3-naphthoyl group found in most indole
derived cannabinoids with the 3-tetramethylcyclopropylmethanone 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 Ki of 0.77nM vs 2,100nM at CB1. It has potent analgesic
and anti-inflammatory
actions in animal models, being especially effective in models of neuropathic pain
, but without producing cannabis-like behavioral effects.
Abbott Laboratories
Abbott Laboratories is an American-based global, diversified pharmaceuticals and health care products company. It has 90,000 employees and operates in over 130 countries. The company headquarters are in Abbott Park, North Chicago, Illinois. The company was founded by Chicago physician, Dr....
which acts as a potent and selective cannabinoid CB2 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...
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...
. Replacing the aromatic 3-benzoyl
Benzoyl
In organic chemistry, benzoyl is the acyl of benzoic acid, with structure C6H5CO-. It should not be confused with benzyl, which is the radical or ion formed from the removal of one of the methyl hydrogens of toluene...
or 3-naphthoyl group found in most indole
Indole
Indole is an aromatic heterocyclic organic compound. It has a bicyclic structure, consisting of a six-membered benzene ring fused to a five-membered nitrogen-containing pyrrole ring. Indole is a popular component of fragrances and the precursor to many pharmaceuticals. Compounds that contain an...
derived cannabinoids with the 3-tetramethylcyclopropylmethanone 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 Ki of 0.77nM vs 2,100nM at CB1. It has potent analgesic
Analgesic
An analgesic is any member of the group of drugs used to relieve pain . The word analgesic derives from Greek an- and algos ....
and anti-inflammatory
Anti-inflammatory
Anti-inflammatory refers to the property of a substance or treatment that reduces inflammation. Anti-inflammatory drugs make up about half of analgesics, remedying pain by reducing inflammation as opposed to opioids, which affect the central nervous system....
actions in animal models, being especially effective in models of neuropathic pain
Neuropathic pain
Neuropathic pain results from lesions or diseases affecting the somatosensory system. It may be associated with abnormal sensations called dysesthesia, which occur spontaneously and allodynia that occurs in response to external stimuli. Neuropathic pain may have continuous and/or episodic ...
, but without producing cannabis-like behavioral effects.
See also
- A-834,735A-834,735A-834,735 is a drug developed by Abbott Laboratories which acts as a potent cannabinoid receptor full agonist at both the CB1 and CB2 receptors, with a Ki of 12nM at CB1 and 0.21nM at CB2...
- A-836,339A-836,339A-836,339 is a drug developed by Abbott Laboratories which acts as a potent cannabinoid receptor full agonist. It is selective for CB2, with Ki values of 0.64nM at CB2 vs 270nM at the psychoactive CB1 receptor, but while it exhibits selective analgesic, anti-inflammatory and anti-hyperalgesic...
- JWH-200JWH-200JWH-200 is an analgesic chemical from the aminoalkylindole family, which acts as a cannabinoid receptor agonist. Its binding affinity at the CB1 receptor is 42nM, around the same as that of THC, but its analgesic potency in vivo was higher than that of other analogues with stronger CB1 binding...
- (1-Pentylindol-3-yl)-(2,2,3,3-tetramethylcyclopropyl)methanone(1-Pentylindol-3-yl)-(2,2,3,3-tetramethylcyclopropyl)methanone-methanone 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. It has high affinity for the CB2 receptor with a Ki of 1.8nM but 83x lower affinity for the CB1...