R-84760 hydrochloride| CAS#157824-23-2 | 157824-29-8 | κ-opioid receptor agonist

MedKoo Cat#: 526991 | Name: R-84760 hydrochloride

Description:

WARNING: This product is for research use only, not for human or veterinary use.

R-84760 is a κ-opioid receptor agonist potentially for the treatment of pain. R-84760 produces an extremely potent antinociceptive effect against tonic pain through the kappa-opioid receptors; the sites of action of subcutaneously administered R-84760 are the supraspinal and spinal loci in the central nervous system; and a part of the mechanism of the antinociceptive effect of R-84760 is activation of the descending noradrenergic pathway.

Chemical Structure

R-84760 hydrochloride

CAS#157824-23-2 (HCl)

Theoretical Analysis

MedKoo Cat#: 526991

Name: R-84760 hydrochloride

CAS#: 157824-23-2 (HCl)

Chemical Formula: C19H25Cl3N2OS

Exact Mass:

Molecular Weight: 435.83

Elemental Analysis: C, 52.36; H, 5.78; Cl, 24.40; N, 6.43; O, 3.67; S, 7.36

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

Bulk Inquiry

Related CAS #

No Data

Synonym

R-84760 hydrochloride; R 84760; R84760; R-86436; R 86436; R86436; R 84761; R-84761; R84761.

IUPAC/Chemical Name

((S)-5,6-dichloro-2,3-dihydro-1H-inden-1-yl)((R)-3-(pyrrolidin-1-ylmethyl)thiomorpholino)methanone hydrochloride

InChi Key

KSUNRZWFIKXTKO-LIOBNPLQSA-N

InChi Code

InChI=1S/C19H24Cl2N2OS.ClH/c20-17-9-13-3-4-15(16(13)10-18(17)21)19(24)23-7-8-25-12-14(23)11-22-5-1-2-6-22;/h9-10,14-15H,1-8,11-12H2;1H/t14-,15+;/m1./s1

SMILES Code

O=C([C@H]1CCC2=C1C=C(Cl)C(Cl)=C2)N3[C@H](CN4CCCC4)CSCC3.[H]Cl

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Related CAS# CAS No. 157824-29-8 (R-84760 Free) 157824-23-2 (R-84760 hydrochloride) Note: R-84760 is the (1R,2S)-isomer; R-86428 is the (1S,2R)-isomer; R-84761 is the (1R,2R)-isomer; R-86436 is the (1S,2S)-isomer.

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 435.83 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Ohsawa M, Kamei J. Modification of kappa-opioid receptor agonist-induced antinociception by diabetes in the mouse brain and spinal cord. J Pharmacol Sci. 2005 May;98(1):25-32. PubMed PMID: 15879680. 2: Mori T, Nomura M, Yoshizawa K, Nagase H, Narita M, Suzuki T. Differential properties between TRK-820 and U-50,488H on the discriminative stimulus effects in rats. Life Sci. 2004 Oct 1;75(20):2473-82. PubMed PMID: 15350822. 3: Zhang Y, Butelman ER, Schlussman SD, Ho A, Kreek MJ. Effect of the kappa opioid agonist R-84760 on cocaine-induced increases in striatal dopamine levels and cocaine-induced place preference in C57BL/6J mice. Psychopharmacology (Berl). 2004 Apr;173(1-2):146-52. PubMed PMID: 14712342. 4: Kobayashi N, Kazui M, Ikeda T. Rapid, real-time sampling of R-84760 in blood by in vivo microdialysis with tandem mass spectrometry. J Pharm Biomed Anal. 2000 Jan;21(6):1233-42. PubMed PMID: 10708407. 5: Kobayashi N, Naganuma H. Quantitative analysis of R-84760, a selective kappa-opioid receptor agonist, in plasma by liquid chromatography with electrospray ionization tandem mass spectrometry. J Pharm Biomed Anal. 1999 May;19(6):829-36. PubMed PMID: 10698548. 6: Fujibayashi K, Kubota K, Saito K. Effects of R-84760, a selective kappa-opioid receptor agonist, on nociceptive reflex in isolated neonatal rat spinal cord. Eur J Pharmacol. 1998 Feb 19;343(2-3):171-7. PubMed PMID: 9570465. 7: Fujibayashi K, Kubota-Watanabe M, Iizuka Y. Effects of R-84760, a selective kappa-opioid receptor agonist, on nociception, locomotion and respiration in rats. Arch Int Pharmacodyn Ther. 1996 Mar-Apr;331(2):153-62. PubMed PMID: 8937626. 8: Fujibayashi K, Iizuka Y. Profiles of the antinociceptive effect of R-84760, a selective kappa-opioid receptor agonist, in the formalin test in mice. Jpn J Pharmacol. 1995 May;68(1):57-63. PubMed PMID: 7494383. 9: Fujibayashi K, Sakamoto K, Watanabe M, Iizuka Y. Pharmacological properties of R-84760, a novel kappa-opioid receptor agonist. Eur J Pharmacol. 1994 Aug 11;261(1-2):133-40. PubMed PMID: 8001635.