Org 28312
Encyclopedia
Org 28312 is a drug developed by Organon International
which acts as a potent cannabinoid receptor
full agonist at both the CB1 and CB2 receptors. It was developed with the aim of finding a water soluble
cannabinoid agonist suitable for intravenous use as an analgesic
, but did not proceed to human trials, with the related compound Org 28611
chosen instead due to its better penetration into the brain. The structure-activity relationship
s of these compounds have subsequently been investigated further leading to the development of a number of more potent analogues, derived by cyclisation around the indole
or piperazine
rings.
Organon International
Organon is a human pharmaceutical company headquartered in Oss, Netherlands. In November 2007 the company became a part of Schering-Plough Corporation, acquired Organon, active pharmaceutical ingredient producer Diosynth , and its veterinary pharmaceutical sister company Intervet from Akzo Nobel. ...
which acts as a potent cannabinoid 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...
full agonist at both the CB1 and CB2 receptors. It was developed with the aim of finding a water soluble
Solubility
Solubility is the property of a solid, liquid, or gaseous chemical substance called solute to dissolve in a solid, liquid, or gaseous solvent to form a homogeneous solution of the solute in the solvent. The solubility of a substance fundamentally depends on the used solvent as well as on...
cannabinoid agonist suitable for intravenous use as an 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 ....
, but did not proceed to human trials, with the related compound Org 28611
Org 28611
Org 28611 is a drug developed by Organon International which acts as a potent cannabinoid receptor full agonist at both the CB1 and CB2 receptors...
chosen instead due to its better penetration into the brain. The structure-activity relationship
Structure-activity relationship
The structure–activity relationship is the relationship between the chemical or 3D structure of a molecule and its biological activity. The analysis of SAR enables the determination of the chemical groups responsible for evoking a target biological effect in the organism...
s of these compounds have subsequently been investigated further leading to the development of a number of more potent analogues, derived by cyclisation around the 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...
or piperazine
Piperazine
Piperazine is an organic compound that consists of a six-membered ring containing two opposing nitrogen atoms. Piperazine exists as small alkaline deliquescent crystals with a saline taste....
rings.