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MedKoo Cat#: 563092 | Name: Detomidine HCl
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Description:

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

Detomidine HCl is an alpha2-Adrenoreceptor agonist with sedative properties.

Chemical Structure

Detomidine HCl
Detomidine HCl
CAS#90038-01-0 (HCl)

Theoretical Analysis

MedKoo Cat#: 563092

Name: Detomidine HCl

CAS#: 90038-01-0 (HCl)

Chemical Formula: C12H15ClN2

Exact Mass: 222.0924

Molecular Weight: 222.71

Elemental Analysis: C, 64.72; H, 6.79; Cl, 15.92; N, 12.58

Price and Availability

Size Price Availability Quantity
50mg USD 350.00 2 Weeks
100mg USD 600.00 2 Weeks
250mg USD 950.00 2 Weeks
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Related CAS #
76631-46-4 (free base) 90038-01-0 (HCl)
Synonym
Detomidine hydrochloride; Detomidine HCl; Domosedan; Dormosedan; MPV 253AII; MPV-253AII; MPV253AII;
IUPAC/Chemical Name
5-[(2,3-Dimethylphenyl)methyl]-1H-imidazole hydrochloride
InChi Key
OIWRDXKNDCJZSM-UHFFFAOYSA-N
InChi Code
InChI=1S/C12H14N2.ClH/c1-9-4-3-5-11(10(9)2)6-12-7-13-8-14-12;/h3-5,7-8H,6H2,1-2H3,(H,13,14);1H
SMILES Code
CC1=C(C)C(CC2=CN=CN2)=CC=C1.[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
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:
Detomidine hydrochloride, an imidazole derivative, is a potent α2-adrenergic agonist that produces dose-dependent sedative and analgesic effects.
In vitro activity:
The in vitro receptor interactions of detomidine, a novel veterinary sedative analgesic, were studied. Detomidine caused a concentration-dependent inhibition of the twitch response in electrically stimulated mouse vas deferens with a pD2 value of 8.8. The effect of detomidine was not antagonized by the opioidergic antagonist naloxone, the dopaminergic antagonist sulpiride, the serotonergic antagonist methysergide, the histamine H2-antagonist cimetidine, the histamine H1-antagonist diphenhydramine and the cholinergic muscarine antagonist atropine. Detomidine produced concentration-dependent contractions of rat anococcygeal muscle and rabbit aortic strips with pD2 values between 2.5 and 6.4. Intrinsic activities (compared to phenylephrine) varied between 0.5 and 0.7. In receptor binding experiments detomidine showed strong affinity to alpha 2-receptors and there was some binding affinity towards alpha 1-receptors. In conclusion, the present results suggest that detomidine is a potent alpha 2-adrenoceptor agonist and that at high concentrations it can also stimulate alpha 1-adrenoceptors. Reference: Eur J Pharmacol. 1985 Jan 22;108(2):163-9. https://pubmed.ncbi.nlm.nih.gov/2984021/
In vivo activity:
Anaesthesia was induced in horses (n = 6) and baseline values were taken after stabilisation of anaesthesia and were statistically compared to values obtained after an intravenous bolus of detomidine (10 micrograms/kg) had been injected at Time 0. Detomidine caused a significant reduction of heart rate (HR), cardiac index (CI), oxygen transport (O2TR) and a significant elevation of the SAPm, systemic vascular resistance (SVR) and coefficient of utilisation of oxygen (O2CU) at 2 min. A significant reduction in HR, CI, SAPm, Hb, content of oxygen in arterial blood (CaO2) and O2TR and a significant elevation of O2CU were observed 10-50 min after the injection of detomidine. Reduction of the isoflurane end-expiratory concentration to 1.3% was followed by a progressive improvement of the SAPm, CI and muscle perfusion towards the baseline values. Further reduction of Hb and CaO2 as compared to the baseline values was observed during the period. The data suggest that detomidine potentiates some of the cardiovascular effects of isoflurane in horses. Reference: J S Afr Vet Assoc. 1996 Dec;67(4):199-203. https://pubmed.ncbi.nlm.nih.gov/9284031/
Solvent mg/mL mM
Solubility
DMSO 63.0 282.88
H2O 20.0 89.90
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 222.71 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. Virtanen R, Nyman L. Evaluation of the alpha 1- and alpha 2-adrenoceptor effects of detomidine, a novel veterinary sedative analgesic. Eur J Pharmacol. 1985 Jan 22;108(2):163-9. doi: 10.1016/0014-2999(85)90721-6. PMID: 2984021. 2. Zullian C, Menozzi A, Pozzoli C, Poli E, Bertini S. Effects of α2-adrenergic drugs on small intestinal motility in the horse: an in vitro study. Vet J. 2011 Mar;187(3):342-6. doi: 10.1016/j.tvjl.2009.12.015. Epub 2010 Jan 22. PMID: 20093057. 3. Steffey EP, Pascoe PJ. Detomidine reduces isoflurane anesthetic requirement (MAC) in horses. Vet Anaesth Analg. 2002 Oct;29(4):223-227. doi: 10.1046/j.1467-2995.2002.00107.x. Epub 2016 Nov 15. PMID: 28404367. 4. Still J, Serteyn D, van der Merwe CA. Cardiovascular and respiratory effects of detomidine in isoflurane-anaesthetised horses. J S Afr Vet Assoc. 1996 Dec;67(4):199-203. PMID: 9284031
In vitro protocol:
1. Virtanen R, Nyman L. Evaluation of the alpha 1- and alpha 2-adrenoceptor effects of detomidine, a novel veterinary sedative analgesic. Eur J Pharmacol. 1985 Jan 22;108(2):163-9. doi: 10.1016/0014-2999(85)90721-6. PMID: 2984021. 2. Zullian C, Menozzi A, Pozzoli C, Poli E, Bertini S. Effects of α2-adrenergic drugs on small intestinal motility in the horse: an in vitro study. Vet J. 2011 Mar;187(3):342-6. doi: 10.1016/j.tvjl.2009.12.015. Epub 2010 Jan 22. PMID: 20093057.
In vivo protocol:
1. Steffey EP, Pascoe PJ. Detomidine reduces isoflurane anesthetic requirement (MAC) in horses. Vet Anaesth Analg. 2002 Oct;29(4):223-227. doi: 10.1046/j.1467-2995.2002.00107.x. Epub 2016 Nov 15. PMID: 28404367. 2. Still J, Serteyn D, van der Merwe CA. Cardiovascular and respiratory effects of detomidine in isoflurane-anaesthetised horses. J S Afr Vet Assoc. 1996 Dec;67(4):199-203. PMID: 9284031.
1: Clarke KW, Taylor PM. Detomidine in horses. Vet Rec. 1985 Dec 21-28;117(25-26):674-5. doi: 10.1136/vr.117.25-26.674. PMID: 4095895. 2: Vainio O. Detomidine. Vet Rec. 1988 Dec 17;123(25):655. PMID: 3218055. 3: da Silva MCC, Ullony KM, de Araújo GR, Jorge-Neto PN, Albuquerque VB, Caramalac SM, de Oliveira AR, Zanella R, Marques MG, Csemark AC, Luczinski TC, Frazílio FO, Silva EVDCE, de Deco-Souza T. Can detomidine replace medetomidine for pharmacological semen collection in domestic cats? Anim Reprod. 2021 Jul 2;18(2):e20210017. doi: 10.1590/1984-3143-AR2021-0017. PMID: 34249155; PMCID: PMC8253561. 4: Alonso B, Carregaro A, Cuypers C, Michielsen A, Gasthuys F, Schauvliege S. Effects of detomidine or romifidine during maintenance and recovery from isoflurane anaesthesia in horses. Vet Anaesth Analg. 2022 Nov;49(6):624-633. doi: 10.1016/j.vaa.2022.07.004. Epub 2022 Jul 19. PMID: 36175293. 5: Bozkan Z, Yaygingul R, Bulut O, Belge A. Measuring the Effects of Detomidine and Medetomidine Alone and in Combination with Ketamine on Tear Production and Intraocular Pressure in Common Buzzards (Buteo buteo). J Avian Med Surg. 2022 Nov;36(3):242-249. doi: 10.1647/21-00064. PMID: 36468801. 6: Pyörälä E, Koppinen J, Vainio O, Alanko M. Detomidine in pregnant cows. Nord Vet Med. 1986 Jul-Aug;38(4):237-40. PMID: 3774525. 7: Mohammad FK, al-Badrany MS, al-Hasan AM. Detomidine-ketamine anaesthesia in chickens. Vet Rec. 1993 Aug 21;133(8):192. doi: 10.1136/vr.133.8.192. PMID: 8236719. 8: Grimsrud KN, Mama KR, Thomasy SM, Stanley SD. Pharmacokinetics of detomidine and its metabolites following intravenous and intramuscular administration in horses. Equine Vet J. 2009 Apr;41(4):361-5. doi: 10.2746/042516409x370900. PMID: 19562897. 9: Bouts T, Dodds J, Berry K, Arif A, Taylor P, Routh A, Gasthuys F. DETOMIDINE AND BUTORPHANOL FOR STANDING SEDATION IN A RANGE OF ZOO-KEPT UNGULATE SPECIES. J Zoo Wildl Med. 2017 Sep;48(3):616-626. doi: 10.1638/2016-0047.1. PMID: 28920785. 10: Dimaio Knych HK, Stanley SD. Pharmacokinetics and pharmacodynamics of detomidine following sublingual administration to horses. Am J Vet Res. 2011 Oct;72(10):1378-85. doi: 10.2460/ajvr.72.10.1378. PMID: 21962281. 11: Chow NS, Seddighi R, Knych HK, Sun X, Doherty TJ. Sedative effects and pharmacokinetics of detomidine when administered intravenously and intravaginally as a gel in alpacas. Vet Anaesth Analg. 2020 Nov;47(6):773-780. doi: 10.1016/j.vaa.2020.07.002. Epub 2020 Jul 27. PMID: 32863105. 12: Dai F, Rausk J, Aspegren J, Huhtinen M, Cannas S, Minero M. Use of Detomidine Oromucosal Gel for Alleviation of Acute Anxiety and Fear in Horses: A Pilot Study. Front Vet Sci. 2020 Oct 20;7:573309. doi: 10.3389/fvets.2020.573309. PMID: 33195566; PMCID: PMC7606972. 13: Cavalero TMS, Papa FO, Schmith RA, Scheeren VFC, Canuto LEF, Gobato MLM, Rodrigues LT, Freitas-Dell'aqua CP. Protocols using detomidine and oxytocin induce ex copula ejaculation in stallions. Theriogenology. 2019 Dec;140:93-98. doi: 10.1016/j.theriogenology.2019.08.024. Epub 2019 Aug 21. PMID: 31454723. 14: Jones DL. Clinical effects of detomidine with or without atropine used for arthrocentesis in horses. Can Vet J. 1993 May;34(5):296-300. PMID: 17424223; PMCID: PMC1686527. 15: Steffey EP, Pascoe PJ. Detomidine reduces isoflurane anesthetic requirement (MAC) in horses. Vet Anaesth Analg. 2002 Oct;29(4):223-227. doi: 10.1046/j.1467-2995.2002.00107.x. Epub 2016 Nov 15. PMID: 28404367. 16: Joubert KE, Briggs P, Gerber D, Gottschalk RG. The sedative and analgesic effects of detomidine-butorphanol and detomidine alone in donkeys. J S Afr Vet Assoc. 1999 Sep;70(3):112-8. doi: 10.4102/jsava.v70i3.769. PMID: 10852680. 17: Clarke KW, Taylor PM. Detomidine: a new sedative for horses. Equine Vet J. 1986 Sep;18(5):366-70. doi: 10.1111/j.2042-3306.1986.tb03655.x. PMID: 3533530. 18: Taylor PM, Browning AP, Harris CP. Detomidine-butorphanol sedation in equine clinical practice. Vet Rec. 1988 Oct 8;123(15):388-90. doi: 10.1136/vr.123.15.388. PMID: 3057722. 19: Gittel C, Brehm W, Wippern M, Roth S, Hillmann A, Michaele A. Xylazine or detomidine in dairy calves: a comparison of clinically relevant pharmacodynamic parameters under sedation. Tierarztl Prax Ausg G Grosstiere Nutztiere. 2021 Feb;49(1):21-29. English. doi: 10.1055/a-1306-3331. Epub 2021 Feb 15. PMID: 33588478. 20: Knych HK, Steffey EP, Stanley SD. The effects of yohimbine on the pharmacokinetic parameters of detomidine in the horse. Vet Anaesth Analg. 2012 May;39(3):221-9. doi: 10.1111/j.1467-2995.2011.00690.x. Epub 2012 Mar 8. PMID: 22405129.