MR2034 | CAS#57236-85-8

MedKoo Cat#: 525795 | Name: MR2034

Description:

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

MR2034 is a kappa-Opioid receptor agonist, stimulating hypothalamic-pituitary-adrenal axis.

Chemical Structure

MR2034

CAS#57236-85-8

Theoretical Analysis

MedKoo Cat#: 525795

Name: MR2034

CAS#: 57236-85-8

Chemical Formula: C19H29NO2

Exact Mass: 303.2198

Molecular Weight: 303.45

Elemental Analysis: C, 75.21; H, 9.63; N, 4.62; O, 10.54

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Synonym

MR2034; MR-2034; MR 2034;

IUPAC/Chemical Name

(2R,11R)-1,2,3,4,5,6-Hexahydro-6,11-dimethyl-3-[[(R)-tetrahydrofuran-2-yl]methyl]-2α,6α-methano-3-benzazocin-8-ol

InChi Key

CDBCMJWTAFNWGY-BVLYKOKCSA-N

InChi Code

InChI=1S/C19H29NO2/c1-13-7-8-20(12-17-4-3-9-22-17)18-10-15-5-6-16(21)11-19(13,15)14(18)2/h5-6,13-14,17-18,21H,3-4,7-12H2,1-2H3/t13?,14-,17+,18+,19?/m0/s1

SMILES Code

OC(C1)=CC=C2C13C(C)CCN(C[C@@H]4OCCC4)[C@]([C@@H]3C)([H])C2

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

Product Data

Product Data

Instruction

View handling instruction

Biological target:

MR2034 is a kappa-Opioid receptor agonist.

In vitro activity:

Accordingly, MR-2034 stimulated hypothalamic CRH release in vitro in a concentration-dependent fashion and this effect was antagonized dose-dependently by MR-1452. Reference: J Neuroendocrinol. 1996 Aug;8(8):579-85. https://pubmed.ncbi.nlm.nih.gov/8866244/

In vivo activity:

MR-2034 was given intravenously to catheterized, freely moving, male Sprague-Dawley rats and serial blood samples were collected for ACTH and corticosterone (B) measurements. We evaluated also the site of MR-2034 action on the HPA axis in vivo, after the administration of alpha-helical CRH9-41, a CRH receptor antagonist, on hypothalamic CRH, pituitary ACTH, and B release in vitro. MR-2034 increased plasma ACTH and B levels in a dose-related fashion and this effect was antagonized by the selective kappa-opioid receptor antagonist MR-1452. In the presence of alpha-helical CRH9-41, the responses of plasma ACTH and B to MR-2034 were blunted significantly, suggesting that this compound activates the HPA axis through a CRH-dependent mechanism. Reference: J Neuroendocrinol. 1996 Aug;8(8):579-85. https://pubmed.ncbi.nlm.nih.gov/8866244/

Preparing Stock Solutions

The following data is based on the product molecular weight 303.45 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

Formulation protocol:

Calogero AE, Scaccianoce S, Burrello N, Nicolai R, Muscolo LA, Kling MA, Angelucci L, D'Agata R. The kappa-opioid receptor agonist MR-2034 stimulates the rat hypothalamic-pituitary-adrenal axis: studies in vivo and in vitro. J Neuroendocrinol. 1996 Aug;8(8):579-85. PMID: 8866244.

In vitro protocol:

In vivo protocol:

1: Rorick-Kehn LM, Witkin JM, Statnick MA, Eberle EL, McKinzie JH, Kahl SD, Forster BM, Wong CJ, Li X, Crile RS, Shaw DB, Sahr AE, Adams BL, Quimby SJ, Diaz N, Jimenez A, Pedregal C, Mitch CH, Knopp KL, Anderson WH, Cramer JW, McKinzie DL. LY2456302 is a novel, potent, orally-bioavailable small molecule kappa-selective antagonist with activity in animal models predictive of efficacy in mood and addictive disorders. Neuropharmacology. 2014 Feb;77:131-44. doi: 10.1016/j.neuropharm.2013.09.021. Epub 2013 Sep 23. PubMed PMID: 24071566. 2: Bowen CA, Negus SS, Zong R, Neumeyer JL, Bidlack JM, Mello NK. Effects of mixed-action kappa/mu opioids on cocaine self-administration and cocaine discrimination by rhesus monkeys. Neuropsychopharmacology. 2003 Jun;28(6):1125-39. Epub 2003 Mar 5. PubMed PMID: 12637953. 3: Wentland MP, Ye Y, Cioffi CL, Lou R, Zhou Q, Xu G, Duan W, Dehnhardt CM, Sun X, Cohen DJ, Bidlack JM. Syntheses and opioid receptor binding affinities of 8-amino-2,6-methano-3-benzazocines. J Med Chem. 2003 Feb 27;46(5):838-49. PubMed PMID: 12593663. 4: Broadbear JH, Negus SS, Butelman ER, de Costa BR, Woods JH. Differential effects of systemically administered nor-binaltorphimine (nor-BNI) on kappa-opioid agonists in the mouse writhing assay. Psychopharmacology (Berl). 1994 Jul;115(3):311-9. PubMed PMID: 7871070. 5: Barg J, Nah SY, Levy R, Saya D, Vogel Z. Modulation of thymidine incorporation by kappa-opioid ligands in rat spinal cord-dorsal root ganglion co-cultures. Brain Res. 1993 Nov 26;629(1):109-14. PubMed PMID: 8287265. 6: Frenk H, Miller J, Johannessen JN, Mayer DJ. Spinal paralysis and catalepsy induced by intrathecal injection of opioid agonists. Pharmacol Biochem Behav. 1990 Jun;36(2):243-7. PubMed PMID: 2162542. 7: Clark JA, Liu L, Price M, Hersh B, Edelson M, Pasternak GW. Kappa opiate receptor multiplicity: evidence for two U50,488-sensitive kappa 1 subtypes and a novel kappa 3 subtype. J Pharmacol Exp Ther. 1989 Nov;251(2):461-8. PubMed PMID: 2553920. 8: Verlinde C, De Ranter C. Assessment of the kappa-opioid activity of a series of 6,7-benzomorphans in the rabbit vas deferens. Eur J Pharmacol. 1988 Aug 9;153(1):83-7. PubMed PMID: 2850928. 9: Hayes AG, Skingle M, Tyers MB. Evaluation of the receptor selectivities of opioid drugs by investigating the block of their effect on urine output by beta-funaltrexamine. J Pharmacol Exp Ther. 1987 Mar;240(3):984-8. PubMed PMID: 3559988. 10: Abbott FV, Franklin KB, Libman RB. A dose-ratio comparison of mu and kappa agonists in formalin and thermal pain. Life Sci. 1986 Nov 24;39(21):2017-24. PubMed PMID: 3023775. 11: Iyengar S, Kim HS, Wood PL. Kappa opiate agonists modulate the hypothalamic-pituitary-adrenocortical axis in the rat. J Pharmacol Exp Ther. 1986 Aug;238(2):429-36. PubMed PMID: 3016237. 12: Chahl LA. Withdrawal responses of guinea-pig isolated ileum following brief exposure to opiates and opioid peptides. Naunyn Schmiedebergs Arch Pharmacol. 1986 Aug;333(4):387-92. PubMed PMID: 2430191. 13: Skingle M, Hayes AG, Tyers MB. Effects of opiates on urine output in the water-loaded rat and reversal by beta-funaltrexamine. Neuropeptides. 1985 Feb;5(4-6):433-6. PubMed PMID: 2987740. 14: Rourke JD, Shaw JS. Failure to demonstrate mu-isoreceptors. Neuropeptides. 1984 Dec;5(1-3):85-8. PubMed PMID: 6099520. 15: Johnson N, Pasternak GW. The binding to rat brain homogenates of Mr2034, a universal opiate. Life Sci. 1983 Sep 5;33(10):985-91. PubMed PMID: 6310291. 16: Tyers MB. A classification of opiate receptors that mediate antinociception in animals. Br J Pharmacol. 1980 Jul;69(3):503-12. PubMed PMID: 6249436; PubMed Central PMCID: PMC2044269.