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Merck
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SML1936

Sigma-Aldrich

Ro 64-6198

≥98% (HPLC)

别名:

(1S,3aS)-8-(2,3,3a,4,5,6-六氢-1H-苯甲醛-1-基)-1-苯基-1,3,8-三氮杂螺[4.5] 癸烷-4-酮, 8-[(1S,3aS)-2,3,3a,4,5,6-六氢-1H-苯甲醛-1-基] -1-苯基-1,3,8-三氮杂螺[4.5] 癸烷-4-酮, Ro64-6198

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About This Item

经验公式（希尔记法）:
C26H31N3O
CAS号:
280783-56-4
分子量:
401.54
MDL號碼:
MFCD04113242
分類程式碼代碼:
12352200
NACRES:
NA.77

品質等級

100

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 2 mg/mL, clear

儲存溫度

2-8°C

SMILES 字串

O=C1C2(CCN([C@]3([H])C4=CC=CC5=C4[C@](CCC5)([H])CC3)CC2)N(C6=CC=CC=C6)CN1

生化／生理作用

Ro 64-6198是一种脑通透性、非肽，高亲和力（相对于0.1 nM OFQ结合人ORL1的Ki = 0.389 nM）痛敏素/孤儿素FQ（N/OFQ）受体ORL-1（KOR-3，NOP）激动剂（通过GTPγS结合测定的EC50 = 38.9 nM；相对于毛喉素刺激的细胞cAMP积累的IC50 = 32.4 nM，比其他阿片受体家族成员有> 100倍的选择性（Ki = 46.8 nM/μ, 89.1 nM/k, 1.38 μM/δ）且对于其他48种受体和离子通道没有显著的亲和力（IC50 >1μM）。在长期给药后，Ro 64-6198可在自发性和条件性焦虑状态（0.3-3.2 mg/kg i.p）的几种大鼠模型中引起ORL1依赖性抗焦虑药作用，而并没有抗惊慌、抗惊厥、镇静、记忆消除活性或对其抗焦虑作用具有耐受性的迹象。

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

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Phillip A Saccone et al.
The Journal of pharmacology and experimental therapeutics, 357(1), 17-23 (2016-01-24)
Nociceptin/orphanin FQ receptor (NOP) agonists have been reported to produce antinociceptive effects in rhesus monkeys with comparable efficacy to μ-opioid receptor (MOP) agonists, but without their limiting side effects. There are also known to be species differences between rodents and
F M Dautzenberg et al.
The Journal of pharmacology and experimental therapeutics, 298(2), 812-819 (2001-07-17)
The novel nonpeptide orphanin FQ/nociceptin (OFQ/N) ligand [(1S,3aS)-8-(2,3,3a,4,5,6-hexahydro-1H-phenalen-1-yl)-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one] (Ro 64-6198) was characterized in vitro and in vivo for its agonistic potential. Ro 64-6198 was 130- to 3500-fold selective for the OFQ/N receptor (ORL1) compared with opiate receptors. In the cAMP
F Jenck et al.
Proceedings of the National Academy of Sciences of the United States of America, 97(9), 4938-4943 (2000-04-12)
The biochemical and behavioral effects of a nonpeptidic, selective, and brain-penetrant agonist at the ORL1 receptor are reported herein. This low molecular weight compound [(1S,3aS)-8- (2,3,3a,4,5, 6-hexahydro-1H-phenalen-1-yl)-1-phenyl-1,3,8-triaza- spiro[4. 5]decan-4-one] has high affinity for recombinant human ORL1 receptors and has 100-fold
Celia Goeldner et al.
Psychopharmacology, 222(2), 203-214 (2012-01-18)
Ro 64-6198, the prototypical non-peptide nociceptin/orphanin FQ peptide (NOP) receptor agonist, has potent anxiolytic-like effects in several preclinical models and species. However the effects of Ro 64-6198 on distinctive anxiety-provoking conditions related to unconditioned conflict behavior as well as its

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