MK-467 HCl

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

MedKoo CAT#: 525685

CAS#: 130466-38-5 (HCl)

Description: MK-467 is a peripheral α2 -adrenoceptor antagonist. MK-467 dose-dependently attenuates the bradycardia associated with dexmedetomidine, and shortens the sedative effect without altering its quality. MK-467 may be useful in attenuating reductions in heart rates alongside dexmedetomidine.

Chemical Structure

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MK-467 HCl
CAS# 130466-38-5 (HCl)
Instruction

Theoretical Analysis

MedKoo Cat#: 525685
Name: MK-467 HCl
CAS#: 130466-38-5 (HCl)
Chemical Formula: C20H27ClN4O4S
Exact Mass: 454.14
Molecular Weight: 454.970
Elemental Analysis: C, 52.80; H, 5.98; Cl, 7.79; N, 12.31; O, 14.07; S, 7.05

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Related CAS #: 114914-42-0 (free base)   130466-38-5 (HCl)    

Synonym: MK467; MK 467; MK-467

IUPAC/Chemical Name: N-(2-((2R,12bS)-2'-oxo-1,3,4,6,7,12b-hexahydrospiro[benzofuro[2,3-a]quinolizine-2,4'-imidazolidin]-3'-yl)ethyl)methanesulfonamide hydrochloride

InChi Key: UTMOWVIYZQWJHT-VASSOYJASA-N

InChi Code: InChI=1S/C20H26N4O4S.ClH/c1-29(26,27)22-8-11-24-19(25)21-13-20(24)7-10-23-9-6-15-14-4-2-3-5-17(14)28-18(15)16(23)12-20;/h2-5,16,22H,6-13H2,1H3,(H,21,25);1H/t16-,20+;/m0./s1

SMILES Code: CS(=O)(NCCN([C@]1(CN2)CCN3CCC4=C(OC5=CC=CC=C54)[C@]3([H])C1)C2=O)=O.[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, not in water

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:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 454.97 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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Honkavaara J, Pypendop B, Turunen H, Ilkiw J. The effect of MK-467, a peripheral α(2) -adrenoceptor antagonist, on dexmedetomidine-induced sedation and bradycardia after intravenous administration in conscious cats. Vet Anaesth Analg. 2016 May 30. doi: 10.1111/vaa.12385. [Epub ahead of print] PubMed PMID: 27238447.
2: de Vries A, Pakkanen SA, Raekallio MR, Ekiri A, Scheinin M, Taylor PM, Vainio OM. Clinical effects and pharmacokinetic variables of romifidine and the peripheral α(2) -adrenoceptor antagonist MK-467 in horses. Vet Anaesth Analg. 2016 Feb 26. doi: 10.1111/vaa.12354. [Epub ahead of print] PubMed PMID: 26918855.
3: Pypendop BH, Honkavaara J, Ilkiw JE. Pharmacokinetics of dexmedetomidine, MK-467, and their combination following intravenous administration in male cats. J Vet Pharmacol Ther. 2016 Feb 20. doi: 10.1111/jvp.12302. [Epub ahead of print] PubMed PMID: 26896345.
4: Bennett RC, Salla KM, Raekallio MR, Hänninen L, Rinne VM, Scheinin M, Vainio OM. Effects of MK-467 on the antinociceptive and sedative actions and pharmacokinetics of medetomidine in dogs. J Vet Pharmacol Ther. 2016 Jan 14. doi: 10.1111/jvp.12292. [Epub ahead of print] PubMed PMID: 26763145.
5: Bennett RC, Hokkanen J, Raekallio MR, Vainio OM. The impact of medetomidine on the protein-binding characteristics of MK-467 in canine plasma. J Vet Pharmacol Ther. 2016 Jan 14. doi: 10.1111/jvp.12291. [Epub ahead of print] PubMed PMID: 26763140.
6: Ruohonen ST, Ranta-Panula V, Bastman S, Chrusciel P, Scheinin M, Streng T. Potentiation of Glibenclamide Hypoglycaemia in Mice by MK-467, a Peripherally Acting Alpha2-Adrenoceptor Antagonist. Basic Clin Pharmacol Toxicol. 2015 Dec;117(6):392-8. doi: 10.1111/bcpt.12440. Epub 2015 Jul 30. PubMed PMID: 26132275.
7: Pakkanen SA, Raekallio MR, Mykkänen AK, Salla KM, de Vries A, Vuorilehto L, Scheinin M, Vainio OM. Detomidine and the combination of detomidine and MK-467, a peripheral alpha-2 adrenoceptor antagonist, as premedication in horses anaesthetized with isoflurane. Vet Anaesth Analg. 2015 Sep;42(5):527-36. doi: 10.1111/vaa.12238. Epub 2014 Dec 22. PubMed PMID: 25529045.
8: Kaartinen J, del Castillo JR, Salla K, Troncy E, Raekallio MR, Vainio OM. Haemodynamic interactions of medetomidine and the peripheral alpha-2 antagonist MK-467 during step infusions in isoflurane-anaesthetised dogs. Vet J. 2014 Nov;202(2):353-60. doi: 10.1016/j.tvjl.2014.08.019. Epub 2014 Aug 22. PubMed PMID: 25201249.
9: Salla K, Restitutti F, Vainionpää M, Junnila J, Honkavaara J, Kuusela E, Raekallio M, Vainio O. The cardiopulmonary effects of a peripheral alpha-2-adrenoceptor antagonist, MK-467, in dogs sedated with a combination of medetomidine and butorphanol. Vet Anaesth Analg. 2014 Nov;41(6):567-74. doi: 10.1111/vaa.12158. Epub 2014 Mar 28. PubMed PMID: 24674053.
10: Salla K, Bennett RC, Restitutti F, Junnila J, Raekallio M, Vainio O. A comparison in dogs of medetomidine, with or without MK-467, and the combination acepromazine-butorphanol as premedication prior to anaesthesia induced by propofol and maintained with isoflurane. Vet Anaesth Analg. 2014 Mar;41(2):163-73. doi: 10.1111/vaa.12094. Epub 2013 Oct 15. PubMed PMID: 24127733.
11: Restitutti F, Laitinen MR, Raekallio MR, Vainionpää M, O'Brien RT, Kuusela E, Vainio OM. Effect of MK-467 on organ blood flow parameters detected by contrast-enhanced ultrasound in dogs treated with dexmedetomidine. Vet Anaesth Analg. 2013 Nov;40(6):e48-56. doi: 10.1111/vaa.12058. Epub 2013 Jun 27. PubMed PMID: 23802592.
12: Vainionpää MH, Raekallio MR, Pakkanen SA, Ranta-Panula V, Rinne VM, Scheinin M, Vainio OM. Plasma drug concentrations and clinical effects of a peripheral alpha-2-adrenoceptor antagonist, MK-467, in horses sedated with detomidine. Vet Anaesth Analg. 2013 May;40(3):257-64. doi: 10.1111/vaa.12012. Epub 2013 Jan 31. PubMed PMID: 23368795.
13: Vainionpää M, Salla K, Restitutti F, Raekallio M, Junnila J, Snellman M, Vainio O. Thermographic imaging of superficial temperature in dogs sedated with medetomidine and butorphanol with and without MK-467 (L-659'066). Vet Anaesth Analg. 2013 Mar;40(2):142-8. doi: 10.1111/j.1467-2995.2012.00768.x. Epub 2012 Aug 14. PubMed PMID: 22891670.
14: Restitutti F, Raekallio M, Vainionpää M, Kuusela E, Vainio O. Plasma glucose, insulin, free fatty acids, lactate and cortisol concentrations in dexmedetomidine-sedated dogs with or without MK-467: a peripheral α-2 adrenoceptor antagonist. Vet J. 2012 Aug;193(2):481-5. doi: 10.1016/j.tvjl.2011.12.010. Epub 2012 Jan 25. PubMed PMID: 22277719.
15: Honkavaara J, Restitutti F, Raekallio M, Salla K, Kuusela E, Ranta-Panula V, Rinne V, Vainio O, Scheinin M. Influence of MK-467, a peripherally acting α2-adrenoceptor antagonist on the disposition of intravenous dexmedetomidine in dogs. Drug Metab Dispos. 2012 Mar;40(3):445-9. doi: 10.1124/dmd.111.042671. Epub 2011 Nov 23. PubMed PMID: 22112381.
16: Honkavaara JM, Restitutti F, Raekallio MR, Kuusela EK, Vainio OM. The effects of increasing doses of MK-467, a peripheral alpha(2)-adrenergic receptor antagonist, on the cardiopulmonary effects of intravenous dexmedetomidine in conscious dogs. J Vet Pharmacol Ther. 2011 Aug;34(4):332-7. doi: 10.1111/j.1365-2885.2010.01242.x. Epub 2010 Oct 25. PubMed PMID: 20969603.
17: Sciberras DG, Reed JW, Elliott C, Blain PG, Goldberg MR. The effects of a peripherally selective alpha 2-adrenoceptor antagonist, MK-467, on the metabolic and cardiovascular response to exercise in healthy man. Br J Clin Pharmacol. 1994 Jan;37(1):39-44. PubMed PMID: 7908531; PubMed Central PMCID: PMC1364707.
18: Warren JB, Dollery CT, Sciberras D, Goldberg MR. Assessment of MK-467, a peripheral alpha 2-adrenergic receptor antagonist, with intravenous clonidine. Clin Pharmacol Ther. 1991 Jul;50(1):71-7. PubMed PMID: 1677320.