SML1936
Ro 64-6198
≥98% (HPLC)
동의어(들):
(1S,3aS)-8-(2,3,3a,4,5,6-Hexahydro-1H-phenalen-1-yl)-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one, 8-[(1S,3aS)-2,3,3a,4,5,6-Hexahydro-1H-phenalen-1-yl]-1-phenyl-1,3,8-Triazaspiro[4.5]decan-4-one, Ro64-6198
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모든 사진(1)
About This Item
실험식(Hill 표기법):
C26H31N3O
CAS Number:
Molecular Weight:
401.54
MDL number:
UNSPSC 코드:
12352200
NACRES:
NA.77
추천 제품
Quality Level
분석
≥98% (HPLC)
양식
powder
색상
white to beige
solubility
DMSO: 2 mg/mL, clear
저장 온도
2-8°C
SMILES string
O=C1C2(CCN([C@]3([H])C4=CC=CC5=C4[C@](CCC5)([H])CC3)CC2)N(C6=CC=CC=C6)CN1
InChI
1S/C26H31N3O/c30-25-26(29(18-27-25)21-9-2-1-3-10-21)14-16-28(17-15-26)23-13-12-20-7-4-6-19-8-5-11-22(23)24(19)20/h1-3,5,8-11,20,23H,4,6-7,12-18H2,(H,27,30)/t20-,23-/m0/s1
생화학적/생리학적 작용
Ro 64-6198 is a brain-penetrant, nonpeptidic, high-affinity (Ki = 0.389 nM against 0.1 nM OFQ for binding human ORL1) nociceptin/orphanin FQ (N/OFQ) receptor ORL-1 (KOR-3, NOP) agonist (EC50 = 38.9 nM by GTPγS binding assay; IC50 = 32.4 nM against forskolin-stimulated cellular cAMP accumulation) with >100-fold selectivity over other opioid receptor family members (Ki = 46.8 nM/μ, 89.1 nM/k, 1.38 μM/δ) and no significant affinity toward 48 other receptors and ion channels (IC50 >1 μM). Ro 64-6198 elicits ORL1-dependent anxiolytic-like effects in several rat models of spontaneous and conditioned anxiety states (0.3-3.2 mg/kg i.p) without antipanic, anticonvulsant, sedative, amnestic activity, or signs of tolerance to its anxiolytic-like effects following chronical dosing.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
가장 최신 버전 중 하나를 선택하세요:
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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