TCS OX2 29 - CAS 372523-75-6
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
Orexin Receptor (OX Receptor)
TCS OX2 29 is a potent and selective OX2 receptor antagonist (IC50 = 40 nM) displaying >250-fold selectivity for OX2 over OX1 and a range of receptors, ion channels and transporters. Orexin is a neuropeptide produced in the lateral hypothalamus (LH) regulates arousal, pain and appetite.
Brife Description:
OX2 receptor antagonist
≥98% by HPLC
(2S)-1-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)-3,3-dimethyl-2-[(4-pyridinylmethyl)amino]-1-butanone hydrochloride
Canonical SMILES:
1.Arousal effects of orexin A on acute alcohol intoxication-induced coma in rats.
Jia X;Yan J;Xia J;Xiong J;Wang T;Chen Y;Qi A;Yang N;Fan S;Ye J;Hu Z Neuropharmacology. 2012 Feb;62(2):775-83. doi: 10.1016/j.neuropharm.2011.08.047. Epub 2011 Sep 10.
The key role of the hypothalamic neuropeptides orexins in maintenance and promotion of arousal has been well established in normal mammalian animals, but whether orexins exert arousal effects under pathological condition such as coma was little studied. In this study, a model of unconscious rats induced by acute alcohol intoxication was used to examine the effects of orexins through intracerebroventricular injection. The results revealed that either orexin A or orexin B induced decrease of duration of loss of right reflex in alcohol-induced unconscious rats. In the presence of the selective orexin receptor 1 antagonist SB 334867 and orexin receptor 2 antagonist TCS OX2 29, the excitatory action of orexin A was completely blocked. Our data further presented that orexin A also induced reduction of delta power in EEG in these rats. Single-unit recording experiment in vivo demonstrated that orexin A could evoke increase of firing activity of prefrontal cortex neurons in unconscious rats. This excitation was completely inhibited by an H(1) receptor antagonist, pyrilamine, whereas application of α(1)-adrenoreceptor antagonist prazosin or 5-HT(2) selective receptor antagonist ritanserin partially attenuated the excitatory effects of orexin A on these neurons.
2.Orexins depolarize rostral ventrolateral medulla neurons and increase arterial pressure and heart rate in rats mainly via orexin 2 receptors.
Huang SC;Dai YW;Lee YH;Chiou LC;Hwang LL J Pharmacol Exp Ther. 2010 Aug;334(2):522-9. doi: 10.1124/jpet.110.167791. Epub 2010 May 21.
An injection of orexin A or B into the cisterna magna or the rostral ventrolateral medulla (RVLM), where bulbospinal vasomotor neurons are located, elevated arterial pressure (AP) and heart rate (HR). We examined how orexins affected RVLM neurons to regulate cardiovascular functions by using in vitro recordings of neuronal activity of the RVLM and in vivo measurement of cardiovascular functions in rats. Orexin A and B concentration-dependently depolarized RVLM neurons. At 100 nM, both peptides excited 42% of RVLM neurons. Tetrodotoxin failed to block orexin-induced depolarization. In the presence of N-(2-methyl-6-benzoxazolyl)-N'-1, 5-naphthyridin-4-yl urea (SB-334867), an orexin 1 receptor (OX(1)R) antagonist, orexin A depolarized 42% of RVLM neurons with a smaller, but not significantly different, amplitude (4.9 +/- 0.8 versus 7.2 +/- 1.1 mV). In the presence of (2S)-1- (3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)-3,3-dimethyl-2-[(4-pyridinylmethyl)amino]-1-butanone hydrochloride (TCS OX2 29), an orexin 2 receptor (OX(2)R) antagonist, orexin A depolarized 25% of RVLM neurons with a significantly smaller amplitude (1.7 +/- 0.5 mV). Coapplication of both antagonists completely eliminated orexin A-induced depolarization.
3.Differential contribution of orexin receptors within the ventral tegmental area to modulation of persistent inflammatory pain.
Ezzatpanah S;Babapour V;Haghparast A Eur J Pain. 2016 Aug;20(7):1090-101. doi: 10.1002/ejp.833. Epub 2016 Feb 12.
BACKGROUND: ;Orexinergic neurons in the lateral hypothalamus (LH) play an important role in pain modulation. In addition, ventral tegmental area (VTA) is known as a part of descending pain modulatory circuitry. Little is known about the interaction between the LH and neural substrates involving in modulation of formalin-induced nociception. Accordingly, we aimed to examine the pain modulatory role of VTA orexin receptors in the formalin test.;METHODS: ;Seventy-eight male Wistar rats were unilaterally implanted with two cannulae above the LH and VTA. Intra-VTA administration of SB-334867 (orexin-1 receptor antagonist) or TCS OX2 29 (orexin-2 receptor antagonist) was performed 5 min before intra-LH microinjection of carbachol (a cholinergic receptor agonist). The procedure was followed by subcutaneous injection of formalin after 5-min interval time.;RESULTS: ;Carbachol attenuated formalin-induced biphasic pain responses and SB-334867 or TCS OX2 29 administration dose-dependently antagonized the LH-induced analgesia during both phases. Blockade of orexin-1 and -2 receptors had more profound effects on the reduction of antinociception during the late phase compared to the early phase. Also, contribution of orexin-1 receptors in mediation of LH-induced analgesia was greater than orexin-2 receptors during the late phase.
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CAS 372523-75-6 TCS OX2 29

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