TCS OX2 29
Chemical Name: (2S)-1-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)-3,3-dimethyl-2-[(4-pyridinylmethyl)amino]-1-butanone hydrochloride
Purity: ≥98%
Biological Activity
TCS OX2 29 is a potent and selective OX2 receptor antagonist (IC50 = 40 nM). Displays >250-fold selectivity for OX2 over OX1 and a range of receptors, ion channels and transporters. Inhibits orexin A induced IP3 accumulation and ERK1/2 phosphorylation in CHO cells transfected with the OX2 receptor.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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Intramolecular fluorescence resonance energy transfer (FRET) sensors of the orexin OX1 and OX2 receptors identify slow kinetics of agonist activation.
Xu TR, Ward RJ, Pediani JD
J. Biol. Chem., 2012;287(18):14937-49. -
Binding kinetics differentiates functional antagonism of orexin-2 receptor ligands.
Mould et al.
Br.J.Pharmacol., 2014;171:351 -
N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: The first orexin-2 receptor selective non-peptidic antagonist.
Hirose et al.
Bioorg.Med.Chem.Lett., 2003;13:4497
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Citations for TCS OX2 29
The citations listed below are publications that use Tocris products. Selected citations for TCS OX2 29 include:
9 Citations: Showing 1 - 9
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Orexin-B exerts excitatory effects on nigral dopaminergic neurons and alleviates motor disorders in MPTP parkinsonian mice
Authors: Bian Et al.
Neurosci Lett 2021;765:136291
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The effect of intracerebroventricular administration of orexin receptor type 2 antagonist on pentylenetetrazol-induced kindled seizures and anxiety in rats.
Authors: Asadi
BMC Neurosci 2018;19(1):49
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Upregulation of orexin receptor in paraventricular nucleus promotes sympathetic outflow in obese Zucker rats.
Authors: Zhou Et al.
Neuropharmacology 2015;99:481
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Both Ox1R and Ox2R orexin receptors contribute to the cardiorespiratory response evoked from the perifornical hypothalamus.
Authors: Beig Et al.
Clin.Exp.Pharmacol.Physiol. 2015;42:1059
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Orexin-A promotes cell migration in cultured rat astrocytes via Ca2+-dependent PKCα and ERK1/2 signals.
Authors: Shu Et al.
PLoS One 2014;9:e95259
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A role for hypocretin/orexin receptor-1 in cue-induced reinstatement of nicotine-seeking behavior.
Authors: Plaza-Zabala Et al.
J Mol Neurosci 2013;38:1724
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Central orexin (hypocretin) 2 receptor antagonism reduces ethanol self-administration, but not cue-conditioned ethanol-seeking, in ethanol-preferring rats.
Authors: Brown Et al.
Int.J.Neuropsychopharmacol. 2013;16:2067
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Orexins/hypocretins acting at Gi protein-coupled OX 2 receptors inhibit cyclic AMP synthesis in the primary neuronal cultures.
Authors: Urbańska Et al.
PLoS One 2012;46:42561
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Orexins depolarize rostral ventrolateral medulla neurons and increase arterial pressure and heart rate in rats mainly via orexin 2 receptors.
Authors: Huang Et al.
J Pharmacol Exp Ther 2010;334:522
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