Drug intelligence / Profile preview

AM630

Development stage
Preclinical
Lead developer
University of Connecticut
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Not Approved For Human Use; Used In Research Via Intraperitoneal Injection In Animal Studies[5].
01

Overview

AM630 (6-Iodopravadoline) is a potent and selective small molecule ligand that acts primarily as an inverse agonist and competitive antagonist at the cannabinoid receptor CB2, with high selectivity over the CB1 receptor. It exhibits a Ki of approximately 31–32 nM for CB2 and is about 165 times more selective for CB2 than for CB1, where it acts as a weak partial agonist. AM630 has been widely used in research to study the physiological roles of cannabinoid receptors—especially CB2—in various systems including pain modulation, inflammation, and neurobiology. It also displays activity at TRPA1 channels in sensory neurons. The compound was one of the first indole-derived cannabinoid ligands substituted at the 6-position of the indole ring—a modification important for affinity and efficacy at both major cannabinoid receptors[1][3][4][7].

Other names
6-Iodopravadolineiodopravadoline
02

Targets

CNR1 (Cannabinoid receptor 1)

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