S-444,823
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S-444,823 is a drug developed by
Shionogi is a Japanese pharmaceutical company best known for developing Crestor. Medical supply and brand name also uses katakana (シオノギ). Shionogi has business roots that date back to 1878, and was incorporated in 1919. Among the medicines pro ...
which is a
cannabinoid Cannabinoids () are several structural classes of compounds found in the cannabis plant primarily and most animal organisms (although insects lack such receptors) or as synthetic compounds. The most notable cannabinoid is the phytocannabinoid tet ...
agonist.Arimura A. Novel Use of Cannabinoid Receptor Agonist. Patent WO 2005/016351
/ref> It was developed as an
antipruritic Antipruritics, abirritants, or anti-itch drugs, are medications that inhibit the itching (Latin: '' pruritus'') often associated with sunburns, allergic reactions, eczema, psoriasis, chickenpox, fungal infections, insect bites and stings like ...
, and has moderate selectivity for the CB2 subtype, having a CB2 affinity of 18nM, and 32x selectivity over the CB1 receptor. In animal studies it showed analgesic effects and strongly reduced itching responses, but without producing side effects such as
sedation Sedation is the reduction of irritability or agitation by administration of sedative drugs, generally to facilitate a medical procedure or diagnostic procedure. Examples of drugs which can be used for sedation include isoflurane, diethyl ether, ...
and
catalepsy Catalepsy (from Ancient Greek , , "seizing, grasping") is a nervous condition characterized by muscular rigidity and fixity of posture regardless of external stimuli, as well as decreased sensitivity to pain. Signs and symptoms Symptoms in ...
that are seen with centrally acting CB1 agonists.


See also

*
JTE 7-31 JTE 7-31 is a selective cannabinoid receptor agonist invented by Japan Tobacco. It is a reasonably highly selective CB2 agonist, but still retains appreciable affinity at CB1, with a Ki of 0.088nM at CB2 vs 11nM at CB1. Legality JTE 7-31 is il ...
* RQ-00202730 *
S-777,469 S-777,469 is a drug developed by Shionogi which is a cannabinoid receptor agonist, with 128x selectivity for the CB2 subtype, having a CB2 affinity of 36nM, and a CB1 affinity over 4600nM. In animal studies it showed antipruritic effects, an ...


References

Cannabinoids Nitrogen heterocycles Thiazoles {{cannabinoid-stub