Detomidine HCl (MPV 253; MPV-253), the hydrochloride salt of detomidine, is an alpha2/α2-Adrenoreceptor agonist with sedative properties. It creates analgesic and sedative effects that are dose-dependent and mediated by α2 catecholamine receptor activation. Detomidine is an imidazole derivative and α2-adrenergic agonist that is mainly used in horses as a large animal sedative. Typically, it can be found as the salt detomidine hydrochloride. Veterinarians can obtain it as a prescription drug under the brand name Dormosedan.

Physicochemical Properties

Molecular Formula	C12H15CLN2
Molecular Weight	222.71
Exact Mass	222.092
Elemental Analysis	C, 64.72; H, 6.79; Cl, 15.92; N, 12.58
CAS #	90038-01-0
Related CAS #	Detomidine; 76631-46-4
PubChem CID	56031
Appearance	White to off-white solid powder
Boiling Point	386.5ºC at 760mmHg
Melting Point	160ºC
Flash Point	200.6ºC
LogP	3.419
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	1
Rotatable Bond Count	2
Heavy Atom Count	15
Complexity	181
Defined Atom Stereocenter Count	0
SMILES	Cl.N1C=C(CC2C(C)=C(C)C=CC=2)NC=1
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
Chemical Name	5-[(2,3-dimethylphenyl)methyl]-1H-imidazole;hydrochloride
Synonyms	MPV 253; MPV253; Detomidine hydrochloride; MPV-253; Detomidine HCl
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	Adrenergic Receptor
ln Vitro	Currently detomidine is only authorized for use on equines. A negative feedback response is induced by α2-adrenergic agonists, which reduce the production of excitatory neurotransmitters and produce dose-dependent analgesic effects through the activation of α2 catecholamine receptors. In addition to its effects on the heart and lungs, detomidine also has an antidiuretic effect and inhibits the sympathetic nervous system.
References	[1]. Pharmacological evidence for the involvement of alpha-2 adrenoceptors in the sedative effect of detomidine, a novel sedative-analgesic. J Vet Pharmacol Ther. 1985 Mar;8(1):30-7. [2]. Cardiovascular and respiratory effects of detomidine in isoflurane-anaesthetised horses. J S Afr Vet Assoc. 1996 Dec;67(4):199-203. . 2019 Jan-Mar;35(1):36-40.
Additional Infomation	See also: Detomidine (has active moiety).

Solubility Data

Solubility (In Vitro)

DMSO: ~45 mg/mL (~202.1 mM) Water: ~45 mg/mL (~202.1 mM) Ethanol: 45 mg/mL

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (11.23 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (11.23 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (11.23 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 4: 140 mg/mL (628.62 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	4.4901 mL	22.4507 mL	44.9014 mL
	5 mM	0.8980 mL	4.4901 mL	8.9803 mL
	10 mM	0.4490 mL	2.2451 mL	4.4901 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.