DETOMIDINE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C12H14N2
Molecular Weight	186.253
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC1=CC=CC(CC2=CNC=N2)=C1C

InChI

InChIKey=RHDJRPPFURBGLQ-UHFFFAOYSA-N

InChI=1S/C12H14N2/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)

HIDE SMILES / InChI

Description
Sources: http://equimed.com/drugs-and-medications/reference/detomidine-hydrochloride |

Detomodine hydrochloride is a sedative with analgesic properties and α2-adrenergic agonist The dose-dependent sedative and analgesic effects reduce production of excitatory neurotransmitters, thereby calming the horse, relieving abdominal pain, and facilitating bronchoscopy and other procedures. Currently, detomidine is only licensed for use in horses.

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Alpha-2 adrenergic receptor 3 Target ID: CHEMBL2111338 Sources: https://www.ncbi.nlm.nih.gov/pubmed/2984021	Agonist 2678

Conditions

Condition	Modality	Targets	Highest Phase	Product
Pain 614 Sources: http://equimed.com/drugs-and-medications/reference/detomidine-hydrochloride	Primary		Approved 8429	Dormosedan Approved Use Unknown

PubMed

Title	Date	PubMed
Laparoscopic closure of the renosplenic space in standing horses.	2001 Nov-Dec	11704952
In vitro effects of oxytocin, acepromazine, detomidine, xylazine, butorphanol, terbutaline, isoproterenol, and dantrolene on smooth and skeletal muscles of the equine esophagus.	2002 Dec	12492290
N-Glucuronidation of some 4-arylalkyl-1H-imidazoles by rat, dog, and human liver microsomes.	2002 Mar	11854148
Serial immobilization of a Brazilian tapir (Tapirus terrestrus) with oral detomidine and oral carfentanil.	2003 Dec	15077719
A comparison of the antinociceptive effects of xylazine, detomidine and romifidine on experimental pain in horses.	2003 Jul	14498850
Flash electroretinography in standing horses using the DTL microfiber electrode.	2003 Mar	12641840
Effects of alpha-2 adrenoceptor agonists during recovery from isoflurane anaesthesia in horses.	2003 Mar	12638794
Effects of intravenous lidocaine on isoflurane concentration, physiological parameters, metabolic parameters and stress-related hormones in horses undergoing surgery.	2003 May	12948155
Standing sedation and pain management for ophthalmic patients.	2004 Aug	15271436
Cumulus expansion, nuclear maturation and connexin 43, cyclooxygenase-2 and FSH receptor mRNA expression in equine cumulus-oocyte complexes cultured in vitro in the presence of FSH and precursors for hyaluronic acid synthesis.	2004 Jun 22	15212696
Overdose during chemical restraint in a black rhinoceros (Diceros bicornis).	2005 Jan	15663740
Effect of defocused CO2 laser on equine tissue perfusion.	2006	16722304
Dissociative anaesthesia during field and hospital conditions for castration of colts.	2006	16722301
Effects of an alveolar recruitment maneuver on cardiovascular and respiratory parameters during total intravenous anesthesia in ponies.	2006 Jan	16426225
Electroencephalographic and electromyographic changes during the use of detomidine and detomidine-butorphanol combination in standing horses.	2006 Mar	16613024
Serial chemical restraint for treatment of decubitus ulcers in two neonatal white rhinoceroses (Ceratotherium simum).	2006 Sep	17319140
A point mutation in a herpesvirus polymerase determines neuropathogenicity.	2007 Nov	17997600
Metabolism before, during and after anaesthesia in colic and healthy horses.	2007 Nov 15	18001483
The cardiopulmonary effects of etorphine, azaperone, detomidine, and butorphanol in field-anesthetized white rhinoceroses (Ceratotherium simum).	2007 Sep	17939346
Development of a composite orthopaedic pain scale in horses.	2008 Oct	18061637
Pharmacokinetics of detomidine and its metabolites following intravenous and intramuscular administration in horses.	2009 Apr	19562897
Effects of dobutamine on cardiac index and arterial blood pressure in isoflurane-anaesthetized horses under clinical conditions.	2009 Aug	19614840
Comparison of the effects of the alpha-2 agonists detomidine, romifidine and xylazine on nociceptive withdrawal reflex and temporal summation in horses.	2009 Jul	19538573
Comparison of azaperone-detomidine-butorphanol-ketamine and azaperone-tiletamine-zolazepam for anaesthesia in piglets.	2009 Mar	19239653
Effect of sedation with detomidine and butorphanol on pulmonary gas exchange in the horse.	2009 May 7	19422714
Histological and immunohistochemical evaluation of autologous cultured bone marrow mesenchymal stem cells and bone marrow mononucleated cells in collagenase-induced tendinitis of equine superficial digital flexor tendon.	2010	20445779
Human exposures to immobilising agents: results of an online survey.	2010 Aug 28	20802186
Immobilization and intravenous anesthesia in a Sumatran rhinoceros (Dicerorhinus sumatrensis).	2010 Mar	20722263
Total intravenous anesthesia with midazolam, ketamine, and xylazine or detomidine following induction with tiletamine, zolazepam, and xylazine in red deer (Cervus elaphus hippelaphus) undergoing surgery.	2010 Oct	20966270

Patents

Sample Use Guides

In Vivo Use Guide

for horses: Oral (gel): 0.04 mg/kg; Intravenous or Intramuscular injection: 0.02-0.04 mg/kg

Route of Administration: Other

In Vitro Use Guide

The sedative alpha2-adrenoceptor agonists medetomidine and detomidine inhibited aldosterone release (range 10-1000 nM). The 4-substituted imidazoles atipamezole, detomidine, and medetomidine inhibited mitochondrial cytochrome P450(11beta/18) in vitro.

Name

Type

Language

DETOMIDINE

Official Name

English

1H-IMIDAZOLE, 4-((2,3-DIMETHYLPHENYL)METHYL)

Common Name

English

detomidine [INN]

Common Name

English

DETOMIDINE [MI]

Common Name

English

4-(2,3-DIMETHYLBENZYL)IMIDAZOLE

Systematic Name

English

Classification Tree Code System Code

WHO-VATC

QN05CM90