MedKoo Cat#: 534671 | Name: Mr 1452

Description:

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

Mr 1452 is a antagonist of morphine and endorphin; kappa opiate receptor antagonist.

Chemical Structure

Mr 1452
Mr 1452
CAS#72656-86-1

Theoretical Analysis

MedKoo Cat#: 534671

Name: Mr 1452

CAS#: 72656-86-1

Chemical Formula: C19H23NO2

Exact Mass: 297.1729

Molecular Weight: 297.40

Elemental Analysis: C, 76.74; H, 7.80; N, 4.71; O, 10.76

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.
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Related CAS #
No Data
Synonym
Mr 1452; Mr1452; Mr-1452
IUPAC/Chemical Name
2,6-Methano-3-benzazocin-8-ol, 3-(3-furanylmethyl)-1,2,3,4,5,6-hexahydro-6,11-dimethyl
InChi Key
MSBGXQSDBDHIGV-UHFFFAOYSA-N
InChi Code
InChI=1S/C19H23NO2/c1-13-18-9-15-3-4-16(21)10-17(15)19(13,2)6-7-20(18)11-14-5-8-22-12-14/h3-5,8,10,12-13,18,21H,6-7,9,11H2,1-2H3
SMILES Code
OC1=CC=C2C(C3(C)CCN(CC4=COC=C4)C(C3C)C2)=C1
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
>3 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

Preparing Stock Solutions

The following data is based on the product molecular weight 297.40 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.

Recalculate based on batch purity %
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: 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. 2: Pilcher CW, Browne JL. Effects of naloxone and Mr 1452 on stress-induced changes in nociception of different stimuli in rats. Life Sci. 1983;33 Suppl 1:697-700. doi: 10.1016/0024-3205(83)90598-2. PMID: 6686642. 3: Machuganska A, Kirov C, Somova L. The effect of naloxone and the kappa antagonist MR 1452 MS on myocardial infarction in rats. Methods Find Exp Clin Pharmacol. 1989 Sep;11(9):559-65. PMID: 2586202. 4: Kraft K, Diehl J, Egen A, Stumpe KO. Chronic kappa-opioid receptor antagonism delays the rise in blood pressure in spontaneously hypertensive rats. Eur J Pharmacol. 1991 Aug 6;200(2-3):219-26. doi: 10.1016/0014-2999(91)90575-b. PMID: 1664325. 5: Ben-Sreti MM, Sewell RD, Upton N. Some observations on the effects of enantiomers of two benzomorphan narcotic antagonists and atropine on analgesia, tremor and hypothermia produced by oxotremorine. Arch Int Pharmacodyn Ther. 1982 Apr;256(2):219-27. PMID: 7103612. 6: Fürst S, Wagner TA, Knoll J. Azidomorphines and heterogenous opiate receptors. Pol J Pharmacol Pharm. 1988 Nov-Dec;40(6):627-34. PMID: 2855884. 7: Ben-Sreti MM, Sewell RD. Stereospecific inhibition of oxotremorine-induced antinociception by (+)-isomers of opioid antagonists: comparison with opioid receptor agonists. J Pharm Pharmacol. 1982 Aug;34(8):501-5. doi: 10.1111/j.2042-7158.1982.tb04773.x. PMID: 6126560. 8: Badawy AA, Aliyu SU. Effects of naloxone and other opiate antagonists on blood-ethanol concentration in acutely-ethanol-intoxicated rats. Neuropeptides. 1985 Feb;5(4-6):341-4. doi: 10.1016/0143-4179(85)90023-x. PMID: 4039802. 9: Siniscalchi A, Bertelli MG, Bianchi C, Beani L. Effect of opioid antagonists on acetylcholine release from guinea-pig brain slices: influence of peptidase inhibition. Pharmacol Res. 1990 Jul-Aug;22(4):493-501. doi: 10.1016/1043-6618(90)90755-3. PMID: 2402481. 10: Bianchi M, Panerai AE. Naloxone-induced analgesia: involvement of kappa- opiate receptors. Pharmacol Biochem Behav. 1993 Sep;46(1):145-8. doi: 10.1016/0091-3057(93)90331-m. PMID: 8255904. 11: Spampinato S, Candeletti S, Cavicchini E, Romualdi P, Speroni E, Ferri S. Antinociceptive activity of salmon calcitonin injected intrathecally in the rat. Neurosci Lett. 1984 Mar 23;45(2):135-9. doi: 10.1016/0304-3940(84)90088-0. PMID: 6547217. 12: Candeletti S, Romualdi P, Spadaro C, Spampinato S, Ferri S. Studies on the antinociceptive effect of intrathecal salmon calcitonin. Peptides. 1985;6 Suppl 3:273-6. doi: 10.1016/0196-9781(85)90385-7. PMID: 3008120. 13: Sacerdote P, Bianchi M, Panerai AE. Involvement of beta-endorphin in the modulation of paw inflammatory edema in the rat. Regul Pept. 1996 Jul 5;63(2-3):79-83. doi: 10.1016/0167-0115(96)00014-6. PMID: 8837214. 14: Parratt JR, Sitsapesan R. Stereospecific antiarrhythmic effect of opioid receptor antagonists in myocardial ischaemia. Br J Pharmacol. 1986 Apr;87(4):621-2. doi: 10.1111/j.1476-5381.1986.tb14577.x. PMID: 3011165; PMCID: PMC1916799. 15: Ventura C, Guarnieri C, Vaona I, Campana G, Pintus G, Spampinato S. Dynorphin gene expression and release in the myocardial cell. J Biol Chem. 1994 Feb 18;269(7):5384-6. PMID: 7906274. 16: Lal KJ, Sewell RD. Possible role for endogenous opiates in the regulation of food intake in the newborn rat. Arch Int Pharmacodyn Ther. 1989 Sep- Oct;301:91-9. PMID: 2624520. 17: Spampinato S, Romualdi P, Candeletti S, Cavicchini E, Ferri S. Distinguishable effects of intrathecal dynorphins, somatostatin, neurotensin and s-calcitonin on nociception and motor function in the rat. Pain. 1988 Oct;35(1):95-104. doi: 10.1016/0304-3959(88)90281-3. PMID: 2904671. 18: Kuhn FJ, Stockhaus K. Prüfung einiger neuer Morphinantagonisten im Tierexperiment [Study on novel morphine antagonists in the animal experiment (author's transl)]. Arzneimittelforschung. 1976;26(11):2009-14. German. PMID: 1037235. 19: Ventura C, Pintus G. Opioid peptide gene expression in the primary hereditary cardiomyopathy of the Syrian hamster. III. Autocrine stimulation of prodynorphin gene expression by dynorphin B. J Biol Chem. 1997 Mar 7;272(10):6699-705. doi: 10.1074/jbc.272.10.6699. PMID: 9045702. 20: Ben-Sreti MM, Gonzalez JP, Sewell RD. Differential effects of SKF 38393 and LY 141865 on nociception and morphine analgesia. Life Sci. 1983;33 Suppl 1:665-8. doi: 10.1016/0024-3205(83)90590-8. PMID: 6607393.