1663564-42-8
Chemical Structure
GAT100
- CAS 番号: 1663564-42-8
- Formula:C25H28N4OS
- Molecular Weight:432.59
IUPAC Name: 3-ethyl-5-isothiocyanato-N-(4-(piperidin-1-yl)phenethyl)-1H-indole-2-carboxamide
InChIKey: YIYLMDVRSNXYOT-UHFFFAOYSA-N
SMILES: O=C(NCCC1=CC=C(C=C1)N2CCCCC2)C=3NC=4C=CC(N=C=S)=CC4C3CC
Biological Activity: GAT100 is a negative allosteric modulator and covalent allosteric probe for cannabinoid receptor type 1 (CB1R). GAT100 acts as a positive allosteric modulator for orthosteric agonist CP55,940 binding to regulate the CB1R signaling pathway. GAT100 reduces the potency and efficacy of orthosteric CB1R agonists in terms of β-arrestin 1 recruitment, phosphorylation of PLCβ3 and ERK1/2, cAMP accumulation, and CB1R internalization. GAT100 is applicable to the research of psychobehavioral and somatic diseases[1][2].
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GAT100 | GAT100 is a negative allosteric modulator and covalent allosteric probe for cannabinoid receptor type 1 (CB1R). GAT100 acts as a positive allosteric modulator for orthosteric agonist CP55,940 binding to regulate the CB1R signaling pathway. GAT100 reduces the potency and efficacy of orthosteric CB1R agonists in terms of β-arrestin 1 recruitment, phosphorylation of PLCβ3 and ERK1/2, cAMP accumulation, and CB1R internalization. GAT100 is applicable to the research of psychobehavioral and somatic diseases. | |||||||||||||||||||||
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- [1]. Kulkarni PM, et al. Novel Electrophilic and Photoaffinity Covalent Probes for Mapping the Cannabinoid 1 Receptor Allosteric Site(s). J Med Chem. 2016;59(1):44-60. [Content Brief]
- [2]. Laprairie RB, et al. Mapping Cannabinoid 1 Receptor Allosteric Site(s): Critical Molecular Determinant and Signaling Profile of GAT100, a Novel, Potent, and Irreversibly Binding Probe. ACS Chem Neurosci. 2016;7(6):776-798. [Content Brief]
Keywords
