DETOMIDINE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C12H14N2
Molecular Weight	186.2534
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

Cc1cccc(Cc2cnc[nH]2)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

Molecular Formula	C12H14N2
Molecular Weight	186.2534
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

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 2 Target ID: CHEMBL2111338 Sources: https://www.ncbi.nlm.nih.gov/pubmed/2984021	Agonist 2470

Conditions

Condition	Modality	Targets	Highest Phase	Product
Pain 580 Sources: http://equimed.com/drugs-and-medications/reference/detomidine-hydrochloride	Primary		Approved 8043	Dormosedan Approved Use Unknown

PubMed

Title	Date	PubMed
Comparison of detomidine and romifidine as premedicants before ketamine and halothane anesthesia in horses undergoing elective surgery.	2001 Mar	11277200
Sedation and chemical restraint of deer.	2002 Dec	16032278
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
The effects of xylazine, detomidine, acepromazine and butorphanol on equine solid phase gastric emptying rate.	2002 Jul	12358052
Epidural morphine and detomidine decreases postoperative hindlimb lameness in horses after bilateral stifle arthroscopy.	2002 May-Jun	11994850
Arthroscopic removal of dorsoproximal chip fractures of the proximal phalanx in standing horses.	2002 May-Jun	11994846
Different contractile effects of alpha1- and alpha2-adrenergic agonists on horse isolated common digital artery smooth muscle ring preparations in vitro.	2002 Oct	12361691
Aberrations in uterine contractile patterns in mares with delayed uterine clearance after administration of detomidine and oxytocin.	2002 Sep	12212889
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
Interleukin-1 (IL-1) system gene expression in granulosa cells: kinetics during terminal preovulatory follicle maturation in the mare.	2003 May 16	12803652
Comparison of etorphine-detomidine and medetomidine-ketamine anesthesia in captive addax (Addax nasomaculatus).	2003 Sep	14582789
Chemical immobilization of captive aardvark (Orycteropus afer).	2004 Dec	15732598
Cardiovascular effects of insufflation of the abdomen with carbon dioxide in standing horses sedated with detomidine.	2004 Mar	15027686
Effects of antitussive agents administered before bronchoalveolar lavage in horses.	2005 Aug	16173487
Accidental human poisoning with a veterinary tranquilliser.	2005 Jul	15983098
Muscle metabolic changes associated with long-term inhalation anaesthesia in the horse analysed by muscle biopsy and microdialysis techniques.	2005 Mar	15737180
Dissociative anaesthesia during field and hospital conditions for castration of colts.	2006	16722301
Gait pattern of the ataxic horse compared to sedated and nonsedated horses.	2006 Aug	17402459
Sedative effects of midazolam and xylazine with or without ketamine and detomidine alone following intranasal administration in Ring-necked Parakeets.	2006 Feb 1	16448361
Clinical observations surrounding an increased incidence of postanesthetic myopathy in halothane-anesthetized horses.	2006 Mar	16476002
Antagonism of detomidine sedation in the horse using intravenous tolazoline or atipamezole.	2006 May	16706278
The effect of hyoscine on dobutamine requirement in spontaneously breathing horses anaesthetized with halothane.	2006 May	16634940
Left- and right-sided laparoscopic-assisted nephrectomy in standing horses with unilateral renal disease.	2007 Aug	17686131
The use of alpha-2 agonists in the equine practice: comparison between three molecules.	2007 Aug	17682902
Radiographic closure time of appendicular growth plates in the Icelandic horse.	2007 Jul 17	17640333
Caries in the infundibulum of the second upper premolar tooth in the horse.	2007 Mar 28	17391523
Sedation with detomidine and acepromazine influences the endoscopic evaluation of laryngeal function in horses.	2007 Nov	18065315
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
Reversible immobilization of asiatic black bear (Ursus thibetanus) with detomidine-tiletamine-zolazepam and atipamezole.	2008 Dec	19110696
Development of a composite orthopaedic pain scale in horses.	2008 Oct	18061637
A comparison of epidural buprenorphine plus detomidine with morphine plus detomidine in horses undergoing bilateral stifle arthroscopy.	2009 Jan	19121161
Analgesic effect of butorphanol in ponies following castration.	2009 Jul	19803050
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
Metabolism during anaesthesia and recovery in colic and healthy horses: a microdialysis study.	2009 Mar 10	19284560
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
Comparison of intraoperative behavioral and hormonal responses to noxious stimuli between mares sedated with caudal epidural detomidine hydrochloride or a continuous intravenous infusion of detomidine hydrochloride for standing laparoscopic ovariectomy.	2010 Aug	20459483
Human exposures to immobilising agents: results of an online survey.	2010 Aug 28	20802186
Tachypnea and antipyresis in febrile horses after sedation with alpha-agonists.	2010 Jul-Aug	20492482
Immobilization and intravenous anesthesia in a Sumatran rhinoceros (Dicerorhinus sumatrensis).	2010 Mar	20722263
Anesthetic management of a white rhinoceros (Ceratotherium simum) undergoing an emergency exploratory celiotomy for colic.	2010 May	20456115
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
Accidental poisoning with detomidine and butorphanol.	2010 Sep	20573843

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.

Substance Class	Chemical Created by `admin` on `Sat Jun 26 04:13:46 UTC 2021` Edited by `admin` on `Sat Jun 26 04:13:46 UTC 2021`
Record UNII	7N8K34P2XH
Record Status	`Validated (UNII)`
Record Version

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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