Orexin 2 Receptor Agonist - CAS 1796565-52-0
Catalog number: 1796565-52-0
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
Orexin Receptor (OX Receptor)
N-[2-[3-[[5-[3-(dimethylcarbamoyl)phenyl]-2-methoxyphenyl]sulfonylamino]anilino]ethyl]-3-methylbenzamide is an orexin 2 receptor agonist that is potentially for the treatment of narcolepsy.
Brife Description:
orexin 2 receptor agonist, narcolepsy
Solid powder
MDK-5220; MDK 5220; MDK5220. Orexin2 receptor agonist; CHEMBL3623075; N-[2-[3-[[5-[3-(dimethylcarbamoyl)phenyl]-2-methoxyphenyl]sulfonylamino]anilino]ethyl]-3-methylbenzamide; GTPL9305; SCHEMBL18138813
Soluble in DMSO.
Store in a cool and dry place and at 0-4 ℃ for short term (days to weeks) or -66 ℃ for long term (months to years).
Shelf Life:
2 years
Canonical SMILES:
1.Role of orexin receptors in the nucleus accumbens in dopamine-dependent turning behaviour of rats.
Kotani A;Ikeda H;Koshikawa N;Cools AR Neuropharmacology. 2008 Mar;54(3):613-9. Epub 2007 Nov 22.
The role of orexin receptors in the nucleus accumbens shell in rat turning behaviour of rats was studied. Unilateral injection of neither the orexin 1 and 2 receptor agonist orexin A (2 microg) nor the orexin 1 receptor antagonist SB 334867 (20 ng) into the nucleus accumbens shell elicited turning behaviour. Unilateral injection of a mixture of dopamine D(1) (SKF 38393) and D2 (quinpirole) receptor agonists into the nucleus accumbens shell has been found to elicit contraversive pivoting. Orexin A (1 and 2 microg) dose-dependently potentiated the contraversive pivoting induced by a mixture of SKF 38393 (1 microg) and quinpirole (10 microg) injected into the nucleus accumbens shell whereas SB 334867 (10 and 20 ng) did not significantly affect the pivoting. The potentiating effect of orexin A (2 microg) on the dopaminergic pivoting was not significantly inhibited by SB 334867 (10 and 20 ng) injected into the nucleus accumbens shell. The contraversive pivoting induced by a mixture of SKF 38393 (1 microg) and quinpirole (10 microg) injected into the nucleus accumbens shell was also potentiated by the orexin 2 receptor agonist orexin B (0.5, 1 and 2 microg), which alone did not elicit turning behaviour.
2.Nonpeptide Orexin-2 Receptor Agonist Attenuates Morphine-induced Sedative Effects in Rats.
Toyama S;Shimoyama N;Tagaito Y;Nagase H;Saitoh T;Yanagisawa M;Shimoyama M Anesthesiology. 2018 May;128(5):992-1003. doi: 10.1097/ALN.0000000000002161.
BACKGROUND: ;Sleepiness and decrease in attention are dose-limiting side effects of opioids. The orexin/hypocretin system plays an important role in maintaining wakefulness. This study aimed to explore the potential of a nonpeptide orexin receptor agonist to alleviate morphine-induced sedative effects.;METHODS: ;Morphine sedative effects were evaluated as changes in electroencephalogram (EEG), locomotor activity, and acoustic startle response in rats (n = 5 to 9 per group). Effects of intracerebroventricular orexin-A and systemic orexin type-2 receptor agonist, YNT-185, on EEG changes induced by morphine were examined. Furthermore, the authors examined effects of morphine administered with or without YNT-185 on locomotor activity and on acoustic startle response.;RESULTS: ;Morphine-induced, frequent, short epochs of increased power (total epoch duration: 0.5 [0.0 to 8.0] s/10 min during baseline vs. 74.0 [49.0 to 115.0] s/10 min during the post-morphine administration period; P = 0.012). EEG analyses revealed that morphine-induced, high-amplitude, slow activity (increase in spectral power of frequencies less than 15 Hz, baseline vs. postmorphine; P < 0.001). Orexin-A and YNT-185 attenuated these changes.
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