WAY 161503 hydrochloride

Names

[ Name ]:
WAY 161503 hydrochloride

[Synonym ]:
8,9-Dichloro-2,3,4,4a-tetrahydro-1H-pyrazino[1,2-a]quinoxalin-5(6H)-one hydrochloride
8,9-DICHLORO-2,3,4,4A-TETRAHYDRO-1H-PYRAZINO[1,2-A]QUINOXALIN-5(6H)-ONE HYDROCHLORIDE

Biological Activity

[Description]:

(Rac)-WAY-161503 hydrochloride is a potent, selective, high affinity 5-HT2C receptor agonist with a Ki of 4 nM and an EC50 of 12 nM. (Rac)-WAY-161503 hydrochloride displays higher affinity for 5-HT2C than 5-HT2A and 5-HT2B receptors. (Rac)-WAY-161503 hydrochloride has anti-obesity and antidepressant effects[1][2].

[Related Catalog]:

Research Areas >> Metabolic Disease

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[Target]

5-HT2C Receptor:4 nM (Ki)

5-HT2C Receptor:12 nM (EC50)

[In Vivo]

(Rac)-WAY-161503 (3-30 mg/kg；腹腔注射；雄性 C57BL/6J 小鼠) hydrochloride 剂量依赖性地降低运动活动，这种作用被 5-HT2C/2B 拮抗剂 SER-082 所阻断[1]。 Animal Model: Male C57BL/6J mice with hallucinogen 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI)[1] Dosage: 3 mg/kg, 10 mg/kg, 30 mg/kg Administration: Intraperitoneal injection (i.p.) Result: Antagonized the PGE2-mediated inhibition of LPS-induced TNF-α release from rat whole blood culture, in a dose-dependent way.

[References]

[1]. Halberstadt AL, et al. 5-HT(2A) and 5-HT(2C) receptors exert opposing effects on locomotor activity in mice. Neuropsychopharmacology. 2009 Jul;34(8):1958-67.

[2]. Welmaker GS, et al. Synthesis and 5-hydroxytryptamine (5-HT) activity of 2,3,4,4a-tetrahydro-1H-pyrazino[1,2-a]quinoxalin-5-(6H)ones and 2,3,4,4a,5,6-hexahydro-1H-pyrazino[1,2-a]quinoxalines. Bioorg Med Chem Lett. 2000 Sep 4;10(17):1991-4.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₁H₁₂Cl₃N₃O

[ Molecular Weight ]:
308.59

[ Exact Mass ]:
307.00500

[ PSA ]:
47.86000

[ LogP ]:
3.00460

MSDS

Click to get detail MSDS

Safety Information

[ RIDADR ]:
NONH for all modes of transport

[ HS Code ]:
2934999090

Customs

[ HS Code ]: 2934999090

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Articles

5-HT(2A) and 5-HT(2C) receptors exert opposing effects on locomotor activity in mice.

Neuropsychopharmacology 34 , 1958-67, (2009)

Although it is well established that hallucinogens act as 5-HT(2A) and 5-HT(2C) receptor agonists, little is known about the relative contributions of 5-HT(2A) and 5-HT(2C) receptors to the acute beha...