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U103

Sigma-Aldrich

U-69593

solid

别名:

(+)-(5α,7α,8β)-N-甲基-N-[7-(1-吡咯烷基)-1-氧杂螺[4,5]癸-8-基]苯乙酰胺, U69593

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About This Item

经验公式（希尔记法）:
C22H32N2O2
CAS号:
96744-75-1
分子量:
356.50
MDL號碼:
MFCD05664586
分類程式碼代碼:
12352200
PubChem物質ID:
24278769
NACRES:
NA.77

形狀

solid

品質等級

100

光學活性

[α]/D +7.8°, c = 0.825 in methanol(lit.)

顏色

white

溶解度

45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: 10 mg/mL
0.1 M HCl: >40 mg/mL
ethanol: >40 mg/mL
0.1 M NaOH: insoluble
H2O: insoluble

儲存溫度

2-8°C

SMILES 字串

CN([C@H]1CC[C@@]2(CCCO2)C[C@@H]1N3CCCC3)C(=O)Cc4ccccc4

InChI

1S/C22H32N2O2/c1-23(21(25)16-18-8-3-2-4-9-18)19-10-12-22(11-7-15-26-22)17-20(19)24-13-5-6-14-24/h2-4,8-9,19-20H,5-7,10-17H2,1H3/t19-,20-,22-/m0/s1

InChI 密鑰

PGZRDDYTKFZSFR-ONTIZHBOSA-N

基因資訊

human ... OPRD1(4985) , OPRK1(4986) , OPRM1(4988)
mouse ... Oprk1(18387)
rat ... Oprd1(24613) , Oprk1(29335) , Oprm1(25601)

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生化／生理作用

U-69593是一种选择性κ阿片受体激动剂。已知U-69593可通过使多巴胺的基础溢流正常化来抑制中肢多巴胺神经元中的可卡因敏化。

特點和優勢

《受体分类和信号转导》手册的 阿片类药物受体页有该化合物的介绍。想要浏览手册的其他页面， 请单击此处。

準備報告

U-69593可溶于45% (w/v) 2-羟丙基-环糊精水溶液（10 mg/ml）、0.1 M HCl（>40 mg/ml）以及乙醇（>40 mg/ml）。然而，它不溶于0.1 M NaOH和水。

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

個人防護裝備

Eyeshields, Gloves, type N95 (US)

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S Stevens Negus et al.
Experimental and clinical psychopharmacology, 16(5), 386-399 (2008-10-08)
Micro opioid receptor agonists are clinically valuable as analgesics; however, their use is limited by high abuse liability. Kappa opioid agonists also produce antinociception, but they do not produce micro agonist-like abuse-related effects, suggesting that they may enhance the antinociceptive
S Stevens Negus et al.
Psychopharmacology, 210(2), 149-159 (2010-01-27)
Selective, centrally acting kappa opioid agonists produce antinociception in a wide range of preclinical assays, but these compounds perform poorly as analgesics in humans. This discrepancy may be related to the behavioral depressant effects of kappa agonists. Kappa antagonists do
Gregory P McLennan et al.
Journal of neurochemistry, 107(6), 1753-1765 (2008-11-19)
GTP binding regulatory protein (G protein)-coupled receptors can activate MAPK pathways via G protein-dependent and -independent mechanisms. However, the physiological outcomes correlated with the cellular signaling events are not as well characterized. In this study, we examine the involvement of
L M Bohn et al.
Journal of neurochemistry, 74(2), 564-573 (2000-01-26)
As reports on G protein-coupled receptor signal transduction mechanisms continue to emphasize potential differences in signaling due to relative receptor levels and cell type specificities, the need to study endogenously expressed receptors in appropriate model systems becomes increasingly important. Here
Karl J Iremonger et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 29(22), 7349-7358 (2009-06-06)
Opioid signaling in the CNS is critical for controlling cellular excitability, yet the conditions under which endogenous opioid peptides are released and the precise mechanisms by which they affect synaptic transmission remain poorly understood. The opioid peptide dynorphin is present
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