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2,2,3,3-Tetramethylcyclopropanecarboxylic acid [3-(2-[ 11 C]methoxyethyl)-4,5-dimethyl-3H-thiazol-(2 Z)-ylidene]amide

2,2,3,3-Tetramethylcyclopropanecarboxylic acid [3-(2-[ 11 C]methoxyethyl)-4,5-dimethyl-3H-thiazol-(2 Z)-ylidene]amide

Kam Leung

PMID: 21290620

Abstract:

There are two subtypes of cannabinoid receptors in mammalian tissues: CB1 and CB2 (1, 2). CB1 receptors are expressed abundantly in neuronal terminals in the central nervous system (CNS) and in some peripheral tissues to inhibit neurotransmitter release. CB1 receptors are found predominately in the striatum, hippocampus, substantia nigra, globus pallidus, and cerebellum. CB2 receptors are present mainly on immune cells in the blood and peripheral tissues (the spleen) to modulate cytokine release (3). However, CB2 receptors have been found in the CNS tissues (neurons and glial cells) at very low levels (4). Both receptor subtypes are coupled through Gi/o proteins to inhibit adenylate cyclase and to modulate potassium and calcium channels. CB1 receptors have been demonstrated to be involved in analgesia, regulation of food intake, and control of movement in normal subjects (3). Alteration of CB1 receptor function has been implicated in a number of human diseases such as depression, schizophrenia, and obesity (5-7). Upregulation of CB2 receptors in the brain is associated with neuroinflammation in disorders such as Alzheimer's disease (AD), multiple sclerosis, encephalitis, and Down's syndrome (8). CB2 receptors are also involved in inflammation associated with pain, osteoporosis, cancer, and liver diseases (9).
Δ9-Tetrahydrocannabinol (THC) is a major active cannabinoid found in marijuana, and it activates CB1 receptors (10). Various radioligands have been developed for imaging of CB1 receptors (11). However, only a few CB2 radioligands have been evaluated in animals as potential positron emission tomography (12) tracers (13-17). 2,2,3,3-Tetramethylcyclopropanecarboxylic acid [3-(2-[11C]methoxyethyl)-4,5-dimethyl-3H-thiazol-(2Z)-ylidene]amide ([11C]A-836339) has been evaluated for use as a CB2 radioligand for brain imaging of neuroinflammation and AD (18). A-836339 is a selective CB2 agonist with high binding (inhibition constant (Ki), 0.64 nM) (19).

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP1134643881	Potassium (2Z)-2-buten-2-yltrifluoroborate		1134643-88-1	Price

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