R-84760 hydrochloride

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

MedKoo CAT#: 526991

CAS#: 157824-23-2 (HCl)

Description: 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.


Price and Availability

Size
Price

Size
Price

Size
Price

R-84760 hydrochloride is not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

img

Theoretical Analysis

MedKoo Cat#: 526991
Name: R-84760 hydrochloride
CAS#: 157824-23-2 (HCl)
Chemical Formula: C19H25Cl3N2OS
Exact Mass:
Molecular Weight: 435.832
Elemental Analysis: C, 52.36; H, 5.78; Cl, 24.40; N, 6.43; O, 3.67; S, 7.36


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

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


Technical Data

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).

Harmonized System Code:
293490


Additional Information

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.


References

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.