Buy Spiradoline (U-62066) Cas 87151-85-7

Buy Spiradoline (U-62066) Cas 87151-85-7

Spiradoline (U-62066) is a drug which acts as a highly selective κ-opioid agonist.^[1] It has analgesic,^[2] diuretic,^[3] and antitussive effects,^[4] and produces subjective effects in animals similar to those of ketazocine and alazocine.^[5] The main effect in humans is sedation, along with analgesic and diuretic effects, but significant side effects such as dysphoria and hallucinations have stopped it from being used clinically. Buy Spiradoline (U-62066) Cas 87151-85-7

• Enadoline

References

• Product Name
  Spiradoline
• Note
  Research use only, not for human use.
• Brief Description
  Spiradoline (U 62066) is a potent, highly selective κ-opioid agonist that has analgesic diuretic and antitussive effects.
• Description
  Spiradoline (U 62066) is a potent, highly selective κ-opioid agonist that has analgesic diuretic and antitussive effects.Pain Phase 2 Discontinued.
• In Vitro
  Using the patch-clamp method in isolated rat cardiac myocytes, indicated that Spiradoline (15 to 500 μM) produces its antiarrythmic effect via blockade of sodium channels (and at the higher doses also of potassium currents) in myocardial tissue. Thus, Spiradoline reduces the peak sodium current, increased the decay rate of the transient outward potassium current, and reduced the sustained plateau potassium amplitude.
• In Vivo
  Spiradoline (U-62066; 0.1-0.4 mg/kg; subcutaneous injection; once; Sprague-Dawley rats) treatment dose-dependently reduces social behaviors in non-stressed adults, producing social avoidance at the highest dose tested, while younger animals displays reduced sensitivity to this socially suppressing effect of Spiradoline. In stressed animals, the socially suppressing effects of the Spiradoline are blunted at all ages, with juveniles and adolescents exhibiting increased social preference in response to certain doses of U-62066. Animal Model:Juvenile, adolescent and adult Sprague-Dawley male and female rats exposured to repeated restraint Dosage:0.1 mg/kg, 0.2 mg/kg, 0.3 mg/kg, and 0.4?mg/kg Administration:Subcutaneous injection; once Result:Dose-dependently reduced social behaviors in non-stressed adults, producing social avoidance at the highest dose tested. Buy Spiradoline (U-62066) Cas 87151-85-7
• Synonyms
  U 62066
• Pathway
  Endocrinology/Hormones
• Target
  Opioid Receptor
• Recptor
  Opioid Receptor
• Research Area
  Neurological Disease
• Indication
  Pain

Chemical Information

• CAS Number
  87151-85-7
• Formula Weight
  425.392
• Molecular Formula
  C22H30Cl2N2O2
• Purity
  >98% (HPLC)
• Solubility
  In Vitro:?DMSO : 50 mg/mL (117.54 mM)
• SMILES
  CN([C@H]1CC[C@@]2(CCCO2)C[C@@H]1N3CCCC3)C(=O)CC4=CC(=C(C=C4)Cl)Cl.CS(=O)(=O)O
• Chemical Name
  2-(3,4-dichlorophenyl)-N-methyl-N-[(5R,7S,8S)-7-pyrrolidin-1-yl-1-oxaspiro[4.5]decan-8-yl]acetamide

Shipping & Storage Information

• Storage
  (-20℃)
• Shipping
  With Ice Pack
• Stability
  ≥ 2 years

Reference

U-62066 is a compound frequently used in research focusing on its binding affinity and action at opioid receptors. In studies pertaining to neuroscience, U-62066 is applied to investigate the modulation of neurotransmitter release and its subsequent effects on neural pathways. This compound is also of interest in examining the role of opioid receptors in the regulation of pain signaling pathways. Additionally, U-62066 is useful for researchers studying the mechanisms of addiction, as it provides a means to understand the complex interactions between neurotransmitter systems and behavior. In biochemistry, U-62066 is employed to study receptor-ligand interactions and to characterize the activation or inhibition of signal transduction processes.

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U-62066 (CAS 87151-85-7) References

1. Comparison of cardiovascular responses to intra-hippocampal mu, delta and kappa opioid agonists in spontaneously hypertensive rats and isolation-induced hypertensive rats.  |  Shen, S. and Ingenito, AJ. 1999. J Hypertens. 17: 497-505. PMID: 10404951
2. Internalization of mu-opioid receptors in rat spinal cord slices.  |  Marvizón, JC., et al. 1999. Neuroreport. 10: 2329-34. PMID: 10439458
3. Effects of a kappa agonist, spiradoline mesylate (U62,066E), on activation and vaginocervical-stimulation produced analgesia in rats.  |  Boyle, TJ., et al. 2001. Brain Res Bull. 54: 213-8. PMID: 11275411
4. Kappa agonist-induced reduction in dopamine release: site of action and tolerance.  |  Donzanti, BA., et al. 1992. Res Commun Chem Pathol Pharmacol. 78: 193-210. PMID: 1282270
5. Central monoaminergic mechanisms in mice and analgesic activity of spiradoline mesylate, a selective kappa-opioid receptor agonist.  |  Kunihara, M., et al. 1992. Eur J Pharmacol. 214: 111-8. PMID: 1325350
6. Roles of different subtypes of opioid receptors in mediating the ventrolateral orbital cortex opioid-induced inhibition of mirror-neuropathic pain in the rat.  |  Zhao, M., et al. 2007. Neuroscience. 144: 1486-94. PMID: 17184926
7. Mu-opioid receptor in the nucleus submedius: involvement in opioid-induced inhibition of mirror-image allodynia in a rat model of neuropathic pain.  |  Wang, JY., et al. 2008. Neurochem Res. 33: 2134-41. PMID: 18473169
8. Role of mu, delta and kappa opioid receptors in ethanol-reinforced operant responding in infant rats.  |  Miranda-Morales, RS., et al. 2012. Behav Brain Res. 234: 267-77. PMID: 22789403
9. Analgesic activity of spiradoline mesylate (U-62,066E), a kappa opioid agonist in mice.  |  Kunihara, M., et al. 1989. Life Sci. 45: 1191-8. PMID: 2796604
10. Quantitative analysis of effects of kappa-opioid agonists on postischemic hippocampal CA1 neuronal necrosis in gerbils.  |  Hall, ED. and Pazara, KE. 1988. Stroke. 19: 1008-12. PMID: 2840759
11. Cardiovascular depressant effects of the kappa opioid receptor agonists U50488H and spiradoline mesylate.  |  Hall, ED., et al. 1988. Circ Shock. 26: 409-17. PMID: 2850873
12. Effects of spiradoline mesylate, a selective kappa-opioid-receptor agonist, on the central dopamine system with relation to mouse locomotor activity and analgesia.  |  Kunihara, M., et al. 1993. Jpn J Pharmacol. 62: 223-30. PMID: 8411771
13. New degradation product of spiradoline mesylate in aqueous solution: formation of an imidazolidine ring.  |  Ogata, M., et al. 1993. J Pharm Sci. 82: 91-4. PMID: 8429499
14. Gender differences in kappa-opioid modulation of cocaine-induced behavior and NMDA-evoked dopamine release.  |  Sershen, H., et al. 1998. Brain Res. 801: 67-71. PMID: 9729284

Spiradoline (U-62066), an arylacetamide, is a selective kappa opioid receptor (KOR) agonist with a Ki of 8.6 nM in guinea pig. The Ki values of Spiradoline for μ and δ receptors are 252 nM and 9400 nM, respectively. Spiradoline has potent diuretic, analgesic, antiarrythmic, antitussive, neuroprotective properties and easily penetrates the blood-brain barrier[1][2].

Using the patch-clamp method in isolated rat cardiac myocytes, indicated that Spiradoline (15 to 500 μM) produces its antiarrythmic effect via blockade of sodium channels (and at the higher doses also of potassium currents) in myocardial tissue. Thus, Spiradoline reduces the peak sodium current, increased the decay rate of the transient outward potassium current, and reduced the sustained plateau potassium amplitude[2].

Spiradoline (U-62066; 0.1-0.4 mg/kg; subcutaneous injection; once; Sprague-Dawley rats) treatment dose-dependently reduces social behaviors in non-stressed adults, producing social avoidance at the highest dose tested, while younger animals displays reduced sensitivity to this socially suppressing effect of Spiradoline. In stressed animals, the socially suppressing effects of the Spiradoline are blunted at all ages, with juveniles and adolescents exhibiting increased social preference in response to certain doses of U-62066[1].

[1]. Elena I Varlinskaya, et al. Stress alters social behavior and sensitivity to pharmacological activation of kappa opioid receptors in an age-specific manner in Sprague Dawley rats. Neurobiol Stress. 2018 Sep 11;9:124-132.
[2]. M-L G Wadenberg. A review of the properties of spiradoline: a potent and selective kappa-opioid receptor agonist. CNS Drug Rev. Summer 2003;9(2):187-98.

Chemical Properties

Cas No.	87151-85-7	SDF
Formula	C22H30Cl2N2O2	M.Wt	425.39
Solubility	DMSO : 50 mg/mL (117.54 mM; Need ultrasonic)	Storage
General tips	Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition	Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
		1 mg	5 mg	10 mg
	1 mM	2.3508 mL	11.7539 mL	23.5078 mL
	5 mM	470.2 μL	2.3508 mL	4.7016 mL
	10 mM	235.1 μL	1.1754 mL	2.3508 mL

Spiradoline (U-62066), an arylacetamide, is a selective kappa opioid receptor (KOR) agonist/activator with a Ki of 8.6 nM in guinea pigs. The Kis of Spiradoline for μ and δ receptors are 252 nM and 9400 nM respectively. Spiradoline has potent diuretic, analgesic, antiarrhythmic, antitussive, neuro-protection effects and readily crosses the BBB (blood-brain barrier).

Biological Activity I Assay Protocols (From Reference)

Targets	Ki: 8.6 nM (κ-opioid receptor in guinea pig), 252 nM (μ-receptor) and 9400 nM (δ-receptor)[2]
ln Vitro	Employing the patch-clamp technique on isolated rat heart myocytes, it was found that spirol (15–500 μM) inhibits potassium currents and sodium channels in cardiac tissue to create its antiarrhythmic activity. At higher concentrations, it also blocks potassium channels. Consequently, spiradoline decreases the sustained plateau potassium amplitude, increases the decay rate of the transient outward potassium current, and decreases the peak sodium current[2].
ln Vivo	In non-stressed adults, Spiradoline (U-62066; 0.1-0.4 mg/kg; subcutaneous injection; once; Sprague-Dawley rats) treatment dose-dependently decreases social behaviors, resulting in social avoidance at the highest dose tested. However, in younger animals, Spiradoline’s socially suppressive effect is less pronounced. The Spiradoline’s socially suppressive effects are attenuated in stressed animals at all ages, with juveniles and adolescents responding to specific dosages of U-62066 with greater social preference[1].
Animal Protocol	Animal/Disease Models: Juvenile, adolescent and adult SD (Sprague-Dawley) male and female rats exposed to repeated restraint[1] Doses: 0.1 mg/kg, 0.2 mg/kg, 0.3 mg/kg, and 0.4 mg/kg Route of Administration: subcutaneous (sc) injection; once Experimental Results: Dose -dependently decreased social behaviors in non-stressed adults, producing social avoidance at the highest dose tested.
References	[1]. Stress alters social behavior and sensitivity to pharmacological activation of kappa opioid receptors in an age-specific manner in Sprague Dawley rats. Neurobiol Stress. 2018 Sep 11;9:124-132. [2]. M-L G Wadenberg. A review of the properties of spiradoline: a potent and selective kappa-opioid receptor agonist. CNS Drug Rev. Summer 2003;9(2):187-98.
Additional Infomation	Spiradoline has been investigated for the basic science of Bipolar Depression.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula	C22H30CL2N2O2
Molecular Weight	425.39
Exact Mass	424.168
CAS #	87151-85-7
Related CAS #	Spiradoline mesylate;87173-97-5
PubChem CID	55652
Appearance	Typically exists as solid at room temperature
LogP	4.498
Hydrogen Bond Donor Count	0
Hydrogen Bond Acceptor Count	3
Rotatable Bond Count	4
Heavy Atom Count	28
Complexity	557
Defined Atom Stereocenter Count	3
SMILES	N([C@H]1CC[C@]2(OCCC2)C[C@@H]1N1CCCC1)(C)C(=O)CC1C=CC(Cl)=C(Cl)C=1
InChi Key	NYKCGQQJNVPOLU-ONTIZHBOSA-N
InChi Code	InChI=1S/C22H30Cl2N2O2/c1-25(21(27)14-16-5-6-17(23)18(24)13-16)19-7-9-22(8-4-12-28-22)15-20(19)26-10-2-3-11-26/h5-6,13,19-20H,2-4,7-12,14-15H2,1H3/t19-,20-,22-/m0/s1
Chemical Name	2-(3,4-dichlorophenyl)-N-methyl-N-[(5R,7S,8S)-7-pyrrolidin-1-yl-1-oxaspiro[4.5]decan-8-yl]acetamide
HS Tariff Code	2934.99.9001
Storage	Powder      -20°C    3 years 4°C     2 years In solvent   -80°C    6 months -20°C    1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO: 50 mg/mL (117.54 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (5.88 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.88 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More Solubility in Formulation 3: ≥ 2.5 mg/mL (5.88 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.    (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.3508 mL	11.7539 mL	23.5078 mL
	5 mM	0.4702 mL	2.3508 mL	4.7016 mL
	10 mM	0.2351 mL	1.1754 mL	2.3508 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Activator of:

1. Peters GR, et al. J Pharmacol Exp Ther. 1987 Jan;240(1):128-31. 2. Kamei J, et al. Eur J Pharmacol. 1990 Oct 9;187(2):281-6. 3. Kunihara M, et al. Life Sci. 1989;45(13):1191-8.

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   Spiradoline (U-62066), an arylacetamide, is a selective kappa opioid receptor (KOR) agonist/activator with a Ki of 8.6 nM in guinea pigs. The Kis of Spiradoline for μ and δ receptors are 252 nM and 9400 …
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