Dexmedetomidine
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MedKoo CAT#: 317594

CAS#: 113775-47-6 (free base)

Description: Dexmedetomidine, sold under the trade names Precedex and Dexdor, among others, is an anxiolytic, sedative, and analgesic medication. Similar to clonidine, it is an agonist of α2-adrenergic receptors in certain parts of the brain. Dexmedetomidine is notable for its ability to provide sedation without risk of respiratory depression (unlike other commonly used sedatives such as propofol, fentanyl, and midazolam) and can provide cooperative or semi-arousable sedation. Dexmedetomidine hydrochloride is also used in veterinary medicine for dogs and cats. The drug was developed by Orion Pharma. (Source: https://en.wikipedia.org/wiki/Dexmedetomidine).


Chemical Structure

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Dexmedetomidine
CAS# 113775-47-6 (free base)

Theoretical Analysis

MedKoo Cat#: 317594
Name: Dexmedetomidine
CAS#: 113775-47-6 (free base)
Chemical Formula: C13H16N2
Exact Mass: 200.13
Molecular Weight: 200.280
Elemental Analysis: C, 77.96; H, 8.05; N, 13.99

Price and Availability

Size Price Availability Quantity
100mg USD 450 2 weeks
200mg USD 750 2 weeks
500mg USD 1450 2 weeks
1g USD 2450 2 weeks
2g USD 3950 2 weeks
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Related CAS #: 145108-58-3 (HCl)   113775-47-6 (free base)    

Synonym: DEXMEDETOMIDINE; Dexmedetomidina; Dexmedetomidinum; MPV 1440; Precedex; Dexdor

IUPAC/Chemical Name: 5-[(1S)-1-(2,3-dimethylphenyl)ethyl]-1H-imidazole

InChi Key: CUHVIMMYOGQXCV-NSHDSACASA-N

InChi Code: InChI=1S/C13H16N2/c1-9-5-4-6-12(10(9)2)11(3)13-7-14-8-15-13/h4-8,11H,1-3H3,(H,14,15)/t11-/m0/s1

SMILES Code: CC1=C(C(=CC=C1)[C@H](C)C2=CN=CN2)C

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:

Product Data:
Biological target: Dexmedetomidine is a sedative medication used by intensive care units and anesthetists that targets the α2 receptor with a Ki of 1.08 nM.
In vitro activity: Primary hippocampal neurons were cultured for 8 days in vitro and pretreated with or without dexmedetomidine or phosphorylation inhibitors prior to propofol exposure. Dexmedetomidine exerts its neuroprotective effect by binding to imidazoline I1 receptors and modulating histone H3 acetylation in dopaminergic neurons in the striatum via the Erk1/2 signaling pathways. In the present study, pretreatment with dexmedetomidine evidently rescued the propofol-induced downregulation of both the BDNF mRNA (Figure 5B) and reduced levels of the p-Erk1/2, p-CREB, and BDNF proteins (Figure 6B–E). No notable difference was observed in the expression of the Erk1/2 and CREB mRNAs and proteins (Figures 5B and 6B–E) in cells pretreated with or without dexmedetomidine. In conclusion, dexmedetomidine alleviates propofol-induced cytotoxicity toward primary hippocampal neurons in vitro, which correlated with the activation of Erk1/2/CREB/BDNF signaling pathways. Reference: Drug Des Devel Ther. 2019 Feb 19;13:695-706. https://pubmed.ncbi.nlm.nih.gov/30858699/
In vivo activity: The antioxidant effects and the mechanism of DEX (dexmedetomidine) were studied in a lipopolysaccharide- (LPS-) induced AKI model in mice. As shown in Figure 1(a), survival rate dropped about 80% in mice subjected to LPS injection within 12 hours and continued to decline sharply starting from 12 hours after sepsis, reaching almost 42% by 120 hours after LPS injection. Intravenous administration of 30 μg/kg and 50 μg/kg DEX extended lifetime and increased survival rate compared with the LPS group (p = 0.038 and p = 0.042). Kidney function was evaluated based on serum Cr and BUN which are the primary indicators of the severity of kidney damage. Levels of BUN and Cr in mice kidneys were significantly higher in the LPS group than in the control group, whereas treatment with DEX decreased serum Cr and BUN levels compared to the LPS group (Figure 1(b)). Furthermore, histological analysis in HE and PAS revealed that mice treated with LPS exhibited severe renal pathological lesions, indicated by widespread tubular necrosis, tubular degeneration, cellular swelling, and inflammatory cell infiltration in renal tissues, whereas DEX treatment significantly reversed these effects (Figure 1(c)). Kidney histology scores in the LPS group were significantly higher than those in the control group, whereas kidney scores in the DEX+LPS group were significantly lower than those in the LPS group. The results suggest that treatment with DEX protects mice from acute kidney injury caused by LPS. Reference: Oxid Med Cell Longev. 2020 Oct 31;2020:5454210. https://pubmed.ncbi.nlm.nih.gov/33194004/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 40.0 199.72
Ethanol 40.0 199.72

Preparing Stock Solutions

The following data is based on the product molecular weight 200.28 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: 1. Yang XM, Liu J, Ji J, Xie J. Effects of dexmedetomidine on the deformability of erythrocytes in vitro and in anesthesia. Exp Ther Med. 2014 Jun;7(6):1631-1634. doi: 10.3892/etm.2014.1633. Epub 2014 Mar 27. PMID: 24926356; PMCID: PMC4043598. 2. Tu Y, Liang Y, Xiao Y, Lv J, Guan R, Xiao F, Xie Y, Xiao Q. Dexmedetomidine attenuates the neurotoxicity of propofol toward primary hippocampal neurons in vitro via Erk1/2/CREB/BDNF signaling pathways. Drug Des Devel Ther. 2019 Feb 19;13:695-706. doi: 10.2147/DDDT.S188436. PMID: 30858699; PMCID: PMC6387615. 3. Li J, Chen Q, He X, Alam A, Ning J, Yi B, Lu K, Gu J. Dexmedetomidine attenuates lung apoptosis induced by renal ischemia-reperfusion injury through α2AR/PI3K/Akt pathway. J Transl Med. 2018 Mar 23;16(1):78. doi: 10.1186/s12967-018-1455-1. PMID: 29566706; PMCID: PMC5865375. 4. Wang Z, Wu J, Hu Z, Luo C, Wang P, Zhang Y, Li H. Dexmedetomidine Alleviates Lipopolysaccharide-Induced Acute Kidney Injury by Inhibiting p75NTR-Mediated Oxidative Stress and Apoptosis. Oxid Med Cell Longev. 2020 Oct 31;2020:5454210. doi: 10.1155/2020/5454210. PMID: 33194004; PMCID: PMC7648709.
In vitro protocol: 1. Yang XM, Liu J, Ji J, Xie J. Effects of dexmedetomidine on the deformability of erythrocytes in vitro and in anesthesia. Exp Ther Med. 2014 Jun;7(6):1631-1634. doi: 10.3892/etm.2014.1633. Epub 2014 Mar 27. PMID: 24926356; PMCID: PMC4043598. 2. Tu Y, Liang Y, Xiao Y, Lv J, Guan R, Xiao F, Xie Y, Xiao Q. Dexmedetomidine attenuates the neurotoxicity of propofol toward primary hippocampal neurons in vitro via Erk1/2/CREB/BDNF signaling pathways. Drug Des Devel Ther. 2019 Feb 19;13:695-706. doi: 10.2147/DDDT.S188436. PMID: 30858699; PMCID: PMC6387615.
In vivo protocol: 1. Li J, Chen Q, He X, Alam A, Ning J, Yi B, Lu K, Gu J. Dexmedetomidine attenuates lung apoptosis induced by renal ischemia-reperfusion injury through α2AR/PI3K/Akt pathway. J Transl Med. 2018 Mar 23;16(1):78. doi: 10.1186/s12967-018-1455-1. PMID: 29566706; PMCID: PMC5865375. 2. Wang Z, Wu J, Hu Z, Luo C, Wang P, Zhang Y, Li H. Dexmedetomidine Alleviates Lipopolysaccharide-Induced Acute Kidney Injury by Inhibiting p75NTR-Mediated Oxidative Stress and Apoptosis. Oxid Med Cell Longev. 2020 Oct 31;2020:5454210. doi: 10.1155/2020/5454210. PMID: 33194004; PMCID: PMC7648709.

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1: Keating GM. Dexmedetomidine: A Review of Its Use for Sedation in the Intensive Care Setting. Drugs. 2015 Jul;75(10):1119-30. doi: 10.1007/s40265-015-0419-5. PMID: 26063213.


2: Persson NDÅ, Uusalo P, Nedergaard M, Lohela TJ, Lilius TO. Could dexmedetomidine be repurposed as a glymphatic enhancer? Trends Pharmacol Sci. 2022 Dec;43(12):1030-1040. doi: 10.1016/j.tips.2022.09.007. Epub 2022 Oct 21. PMID: 36280451.


3: Barends CR, Absalom A, van Minnen B, Vissink A, Visser A. Dexmedetomidine versus Midazolam in Procedural Sedation. A Systematic Review of Efficacy and Safety. PLoS One. 2017 Jan 20;12(1):e0169525. doi: 10.1371/journal.pone.0169525. PMID: 28107373; PMCID: PMC5249234.


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7: Mahmoud M, Mason KP. Dexmedetomidine: review, update, and future considerations of paediatric perioperative and periprocedural applications and limitations. Br J Anaesth. 2015 Aug;115(2):171-82. doi: 10.1093/bja/aev226. PMID: 26170346.


8: Chima AM, Mahmoud MA, Narayanasamy S. What Is the Role of Dexmedetomidine in Modern Anesthesia and Critical Care? Adv Anesth. 2022 Dec;40(1):111-130. doi: 10.1016/j.aan.2022.06.003. PMID: 36333042.


9: Carr ZJ, Cios TJ, Potter KF, Swick JT. Does Dexmedetomidine Ameliorate Postoperative Cognitive Dysfunction? A Brief Review of the Recent Literature. Curr Neurol Neurosci Rep. 2018 Aug 6;18(10):64. doi: 10.1007/s11910-018-0873-z. PMID: 30083844.


10: Kawazoe Y, Miyamoto K, Morimoto T, Yamamoto T, Fuke A, Hashimoto A, Koami H, Beppu S, Katayama Y, Itoh M, Ohta Y, Yamamura H; Dexmedetomidine for Sepsis in Intensive Care Unit Randomized Evaluation (DESIRE) Trial Investigators. Effect of Dexmedetomidine on Mortality and Ventilator-Free Days in Patients Requiring Mechanical Ventilation With Sepsis: A Randomized Clinical Trial. JAMA. 2017 Apr 4;317(13):1321-1328. doi: 10.1001/jama.2017.2088. PMID: 28322414; PMCID: PMC5469298.


11: Duan X, Coburn M, Rossaint R, Sanders RD, Waesberghe JV, Kowark A. Efficacy of perioperative dexmedetomidine on postoperative delirium: systematic review and meta-analysis with trial sequential analysis of randomised controlled trials. Br J Anaesth. 2018 Aug;121(2):384-397. doi: 10.1016/j.bja.2018.04.046. Epub 2018 Jun 22. PMID: 30032877.


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13: Jun JH, Kim KN, Kim JY, Song SM. The effects of intranasal dexmedetomidine premedication in children: a systematic review and meta-analysis. Can J Anaesth. 2017 Sep;64(9):947-961. English. doi: 10.1007/s12630-017-0917-x. Epub 2017 Jun 21. PMID: 28639236.


14: Qiu Z, Lu P, Wang K, Zhao X, Li Q, Wen J, Zhang H, Li R, Wei H, Lv Y, Zhang S, Zhang P. Dexmedetomidine Inhibits Neuroinflammation by Altering Microglial M1/M2 Polarization Through MAPK/ERK Pathway. Neurochem Res. 2020 Feb;45(2):345-353. doi: 10.1007/s11064-019-02922-1. Epub 2019 Dec 10. PMID: 31823113.


15: Poon WH, Ling RR, Yang IX, Luo H, Kofidis T, MacLaren G, Tham C, Teoh KLK, Ramanathan K. Dexmedetomidine for adult cardiac surgery: a systematic review, meta-analysis and trial sequential analysis. Anaesthesia. 2023 Mar;78(3):371-380. doi: 10.1111/anae.15947. Epub 2022 Dec 19. PMID: 36535747.


16: Mantz J, Josserand J, Hamada S. Dexmedetomidine: new insights. Eur J Anaesthesiol. 2011 Jan;28(1):3-6. doi: 10.1097/EJA.0b013e32833e266d. PMID: 20881501.


17: Burlacu CC, Neag MA, Mitre AO, Sirbu AC, Badulescu AV, Buzoianu AD. The Role of miRNAs in Dexmedetomidine's Neuroprotective Effects against Brain Disorders. Int J Mol Sci. 2022 May 13;23(10):5452. doi: 10.3390/ijms23105452. PMID: 35628263; PMCID: PMC9141783.


18: Nair AS, Saifuddin MS, Naik V, Rayani BK. Dexmedetomidine in cancer surgeries: Present status and consequences with its use. Indian J Cancer. 2020 Jul-Sep;57(3):234-238. doi: 10.4103/ijc.IJC_376_19. PMID: 32769293.


19: Vorobeichik L, Brull R, Abdallah FW. Evidence basis for using perineural dexmedetomidine to enhance the quality of brachial plexus nerve blocks: a systematic review and meta-analysis of randomized controlled trials. Br J Anaesth. 2017 Feb;118(2):167-181. doi: 10.1093/bja/aew411. PMID: 28100520.


20: Wang W, Ma Y, Liu Y, Wang P, Liu Y. Effects of Dexmedetomidine Anesthesia on Early Postoperative Cognitive Dysfunction in Elderly Patients. ACS Chem Neurosci. 2022 Aug 3;13(15):2309-2314. doi: 10.1021/acschemneuro.2c00173. Epub 2022 Jul 21. PMID: 35864562.