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品質等級
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
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
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
Zhenlong Li et al.
The international journal of neuropsychopharmacology, 26(7), 483-495 (2023-06-07)
BTRX-246040, a nociceptin/orphanin FQ peptide receptor antagonist, is being developed for the treatment of depressive patients. However, the underlying mechanism of this potential antidepressant is still largely unclear. Here, we studied the antidepressant-related actions of BTRX-246040 in the ventrolateral periaqueductal
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
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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