GR 89696 fumarate

Names

[ CAS No. ]:
126766-32-3

[ Name ]:
GR 89696 fumarate

Biological Activity

[Description]:

GR 89696 is a highly selective κ2 opioid receptor agonist with potential to prevent pruritus[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Opioid Receptor

Research Areas >> Inflammation/Immunology

Signaling Pathways >> Neuronal Signaling >> Opioid Receptor

[In Vivo]

GR 89696 (intramuscular injection, 0.01-0.1 μg/kg) 可以以一种剂量依赖的方式减轻鞘内注射吗啡（0.03mg)诱导的抓挠反应而不影响吗啡镇痛作用[1]。 GR-896960(subcutaneous injection, 1 mg/kg) 在大鼠永久性局灶性缺血模型中，使大脑动脉梗塞体积减少了 38%[2]。

[References]

[1]. Mei-Chuan Ko, et al. Effects of atypical kappa-opioid receptor agonists on intrathecal morphine-induced itch and analgesia in primates. J Pharmacol Exp Ther. 2009 Jan;328(1):193-200.

[2]. A Barber, et al. Effects of GR-89696 and the novel peripherally selective OP2 agonists, EMD-61569 and EMD-61747, against focal cerebral ischemia in the rat. Methods Find Exp Clin Pharmacol. 1999 Mar;21(2):105-13

Chemical & Physical Properties

[ Boiling Point ]:
559.2ºC at 760 mmHg

[ Molecular Formula ]:
C₂₃H₂₉Cl₂N₃O₇

[ Molecular Weight ]:
530.39800

[ Flash Point ]:
292ºC

[ Exact Mass ]:
529.13800

[ PSA ]:
127.69000

[ LogP ]:
2.43640

[ Vapour Pressure ]:
1.55E-12mmHg at 25°C

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

Articles

[11C]GR103545: novel one-pot radiosynthesis with high specific activity.

Nucl. Med. Biol. 38(2) , 215-21, (2011)

GR103545 is a potent and selective kappa-opioid receptor agonist. Previous studies in non-human primates demonstrated favorable properties of [(11)C]GR103545 as a positron emission tomography tracer f...

GR89,696: a potent kappa-opioid agonist with subtype selectivity in rhesus monkeys.

J. Pharmacol. Exp. Ther. 298(3) , 1049-59, (2001)

GR89,696 is a synthetic kappa-opioid receptor agonist, recently reported to have an agonist profile consistent with selectivity at the proposed "kappa(2)" subtype. The present studies evaluated the ef...

[(11)C]-GR89696, a potent kappa opiate receptor radioligand; in vivo binding of the R and S enantiomers.

Nucl. Med. Biol. 29(1) , 47-53, (2002)

The R and S enantiomers of [(11)C]GR89696, [(11)C]-methyl 4-[(3,4-dichlorophenyl)acetyl]-3-[(1-pyrrolidinyl)methyl]-1-piperazinecarboxylate, were synthesized from their appropriate chiral precursors a...

Related Compounds

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