CP 376395 hydrochloride
Chemical Name: N-(1-Ethylpropyl)-3,6-dimethyl-2-(2,4,6-trimethylphenoxy)-4-pyridinamine hydrochloride
Purity: ≥99%
Biological Activity
CP 376395 hydrochloride is a potent and selective CRF1 receptor antagonist (Ki values are 12 and >10000 nM for CRF1 and CRF2 receptors respectively). Binds at an allosteric site. Attenuates CRF-induced activation of the HPA axis in vivo following i.v. administration. Orally active.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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2-Aryloxy-4-alkylaminopyridines: discovery of novel corticotropin-releasing factor 1 antagonists.
Chen et al.
J.Med.Chem., 2008;51:1385 -
Structure of class B GPCR corticotropin-releasing factor receptor 1.
Hollenstein et al.
Nature, 2013;499:438 -
Small molecule allosteric modulators of G-protein-coupled receptors: drug-target interactions.
Lu et al.
J.Med.Chem., 2019;62:24 -
Prenatal betamethasone exposure increases corticotropin-releasing hormone expression along with increased hippocampal slice excitability in the developing hippocampus
MJ Benson, M Lauková, K Borges, J Velíšková, L Velíšek
Epilepsy Res., 2020;160(0):106276.
Product Datasheets
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Citations for CP 376395 hydrochloride
The citations listed below are publications that use Tocris products. Selected citations for CP 376395 hydrochloride include:
3 Citations: Showing 1 - 3
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Conformational thermostabilisation of cortico. releasing factor receptor 1.
Authors: Kean Et al.
Mol Pain 2015;5:11954
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Importance of CRF receptor-mediated mechanisms of the bed nucleus of the stria terminalis in the processing of anxiety and pain.
Authors: Tran Et al.
Neuropsychopharmacology 2014;39:2633
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Social stress and CRF-DA interactions in the VTA: role in long-term escalation of cocaine self-administration.
Authors: Boyson Et al.
J Neurosci 2014;34:6659
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