1. GPCR/G Protein Neuronal Signaling
  2. Opioid Receptor
  3. U-69593

U-69593 is a potent and selective κ1-opioid receptor agonist. U-69593 attenuates addictive agent-induced behavioral sensitization in the rat. U-69593 reduces anxiety and enhances spontaneous alternation memory in mice. U-69593 reduces calcium-dependent dialysate levels of dopamine and glutamate in the ventral striatum.

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U-69593 Chemical Structure

U-69593 Chemical Structure

CAS No. : 96744-75-1

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Based on 1 publication(s) in Google Scholar

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Description

U-69593 is a potent and selective κ1-opioid receptor agonist[1]. U-69593 attenuates addictive agent-induced behavioral sensitization in the rat[2]. U-69593 reduces anxiety and enhances spontaneous alternation memory in mice[3]. U-69593 reduces calcium-dependent dialysate levels of dopamine and glutamate in the ventral striatum[4].

IC50 & Target

κ Opioid Receptor/KOR

 

In Vivo

U-69593 (0.16 mg/kg; s.c.) attenuates addictive agent-induced behavioral sensitization in the rat[2].
U-69593 (1, 10, 25 nmol/μL; Microinjection) reduces anxiety and enhances spontaneous alternation memory in mice[3].
U-69593 (0.32 mg/kg; s.c.) decreases acute amphetamine-evoked behaviors and calcium-dependent dialysate levels of dopamine and glutamate in the ventral striatum[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Rat[2]
Dosage: 0.16 mg/kg
Administration: S.c. (an acute injection of cocaine (20 mg/kg i.p.))
Result: Attenuated the acute and chronic effects of cocaine on locomotor activity and stereotypy.
Animal Model: CD-1 mice[3]
Dosage: 1, 10, 25 nmol/µL
Administration: Microinjection (in the infralimbic cortex (IL)), once every week, 2 weeks
Result: Dose-dependently prolonged transfer-latency (T-L) and produced a dose-dependent anxiolytic behavioural profile, and after 24 h, the mouse were observed small but detectable carry-over effects. In week 2, U-69593 dose-dependently prolonged T/L and produced an anxiolytic behavioural profile in the first EPM (elevated plus-maze) trial, but observed a robust anxiolytic behavioural profile.
Animal Model: 280-350 g, male Wistar rats[4]
Dosage: 0.32 mg/kg
Administration: S.c. (followed 15 min later by an injection of amphetamine (2.5 mg/kg i.p.))
Result: Significantly reduced the amphetamine-stimulated increase in dialysate dopamine levels and blocked the ability of amphetamine to evoke an increase in dialysate glutamate levels.
Molecular Weight

356.50

Formula

C22H32N2O2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CN([C@@H]1[C@](N2CCCC2)([H])C[C@]3(CCCO3)CC1)C(CC4=CC=CC=C4)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

45% SBE-β-CD in saline : ≥ 10 mg/mL (28.05 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8050 mL 14.0252 mL 28.0505 mL
5 mM 0.5610 mL 2.8050 mL 5.6101 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation

Purity: ≥99.0%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
45% SBE-β-CD in saline 1 mM 2.8050 mL 14.0252 mL 28.0505 mL 70.1262 mL
5 mM 0.5610 mL 2.8050 mL 5.6101 mL 14.0252 mL
10 mM 0.2805 mL 1.4025 mL 2.8050 mL 7.0126 mL
15 mM 0.1870 mL 0.9350 mL 1.8700 mL 4.6751 mL
20 mM 0.1403 mL 0.7013 mL 1.4025 mL 3.5063 mL
25 mM 0.1122 mL 0.5610 mL 1.1220 mL 2.8050 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
U-69593
Cat. No.:
HY-12363
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