An allosteric modulator of the CB1 receptor; the S-(–) enantiomer of GAT211; enhances the binding of CP 55

GAT229 – 5 mg

Brand:
Cayman
CAS:
889860-85-9
Storage:
-20
UN-No:
Non-Hazardous - /

GAT229 is a positive allosteric modulator of cannabinoid receptor 1 (CB1) and the S-(–) enantiomer of the CB1 modulator GAT211.{35179,48089} It does not activate the receptor on its own but enhances the binding and activity of CB agonists. GAT229 (1 µM) enhances the binding of the CB1 full agonist CP 55,940 to CHO cells expressing human recombinant CB1 (hCB1), as well as the activity of 2-arachidonoyl glycerol (2-AG; Item No. 62160), arachidonoyl ethanolamide (AEA; Item No. 90050), and CP 55,940 in arrestin2 recruitment assays and increases ERK1/2 and PLCβ3 phosphorylation in HEK293 cells expressing hCB1. GAT229 (1 μM) enhances depolarization-induced suppression of excitation but does not inhibit excitatory postsynaptic currents (EPSCs) in murine autaptic hippocampal neurons.{48089} GAT229 (0.2%, topical) reduces intraocular pressure by 5.8 and 7.7 mm Hg after 6 and 12 hours, respectively, in a transgenic mouse model of ocular hypertension using nose, ear, eye mutation (nee) mice.{48090}  

 

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Description

An allosteric modulator of the CB1 receptor; the S-(–) enantiomer of GAT211; enhances the binding of CP 55,940 to CHO cells expressing hCB1 by 130% at 1 μM; enhances the activity of 2-AG, AEA, and CP 55,940 in arrestin2, as well as ERK1/2 and PLCβ3 phosphorylation, assays to HEK293 cells expressing hCB1; enhances depolarization-induced suppression of excitation but does not inhibit excitatory postsynaptic currents in murine autaptic hippocampal neurons at 1 μM; reduces intraocular pressure by 5.8 and 7.7 mm Hg after 6 and 12 hours, respectively, in a nee transgenic mouse model of ocular hypertension at 0.2%, topical

Formal name: 3-[(1S)-2-nitro-1-phenylethyl]-2-phenyl-1H-indole

Synonyms: 

Molecular weight: 342.4

CAS: 889860-85-9

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Receptor Pharmacology|Allosteric Modulators||Research Area|Neuroscience|Cannabinoid Research|CB1 & CB2 Receptors||Research Area|Neuroscience|Cannabinoid Research|Endocannabinoids||Research Area|Neuroscience|Ophthalmology

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