Details
Stereochemistry | RACEMIC |
Molecular Formula | C13H16N2.ClH |
Molecular Weight | 236.74 |
Optical Activity | ( + / - ) |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CC(C1=CN=CN1)C2=C(C)C(C)=CC=C2
InChI
InChIKey=VPNGEIHDPSLNMU-UHFFFAOYSA-N
InChI=1S/C13H16N2.ClH/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);1H
DescriptionSources: http://www.ekavet.com/veterinary-medications/425-domitor-1-mg-ml-solution-for-injectionCurator's Comment: description was created based on several sources, including
http://www.ncbi.nlm.nih.gov/pubmed/2571177
Sources: http://www.ekavet.com/veterinary-medications/425-domitor-1-mg-ml-solution-for-injection
Curator's Comment: description was created based on several sources, including
http://www.ncbi.nlm.nih.gov/pubmed/2571177
Domitor (medetomidine hydrochloride) is indicated for use in dogs: for restraint, sedation and analgesia associated with clinical examinations and procedures, minor surgery, pre-anaesthesia and as a premedicant before thiopentone-halothane general a naesthesiaand as a premedicant before general anaesthesia with propofol. In combination with butorphanol for sedation and analgesia, and as a premedicant prior to thiopentone anaesthesia. In cats: for restraint and sedation. Medetomidine is a potent and highly selective alpha2-adrenoreceptor agonist with both central and peripheral activity, and acting both presynaptically and postsynaptically. Its primary effects are sedative and analgesic resulting from its central depressant activity. It has no local anaesthetic properties. Like other compounds of its class there are secondary effects, including bradycardia. Blood pressure is increased but then returns to normal or just below. Body temperature is decreased in a dose dependent manner and intestinal motility is also reduced. The drug has been developed by Orion Pharma. It is currently approved for dogs in the United States, and distributed in the United States by Pfizer Animal Health and by Novartis Animal Health in Canada under the product name Domitor. The marketed product is a racemic mixture of two stereoisomers; dexmedetomidine is the isomer with more useful effects, and is now marketed as Dexdomitor.
CNS Activity
Sources: http://www.ekavet.com/veterinary-medications/425-domitor-1-mg-ml-solution-for-injection
Curator's Comment: Medetomidine is a potent and highly selective alpha2-adrenoreceptor agonist with both central and peripheral activity, and acting both presynaptically and postsynaptically. Its primary effects are sedative and analgesic resulting from its central depressant activity. It has no local anaesthetic properties
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL2095158 Sources: http://www.ncbi.nlm.nih.gov/pubmed/2571177 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | DOMITOR Approved UseDogs: For restraint, sedation and analgesia associated with clinical examinations and procedures, minor surgery, pre-anaesthesia and as a premedicant before thiopentone-halothane general a naesthesiaand as a premedicant before general anaesthesia with propofol.
Cats: For restraint and sedation. |
PubMed
Title | Date | PubMed |
---|---|---|
Comparison of neurologic responses to the use of medetomidine as a sole agent or preanesthetic in laboratory beagles. | 1992 |
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Postoperative analgesic and cardiopulmonary effects in dogs of oxymorphone administered epidurally and intramuscularly, and medetomidine administered epidurally: a comparative clinical study. | 1996 Jul-Aug |
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Reduced blood flow and oxygenation in SA-1 tumours after electrochemotherapy with cisplatin. | 2002 Oct 21 |
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Regulation of Cl- secretion by alpha2-adrenergic receptors in mouse colonic epithelium. | 2003 Apr 15 |
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[Domitor not to used in collies?]. | 2003 May 15 |
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The effect of cartilage and bone density of mushroom-shaped, photooxidized, osteochondral transplants: an experimental study on graft performance in sheep using transplants originating from different species. | 2005 Dec 15 |
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Evaluation of two combinations of Domitor, Zoletil 100, and Euthatal to obtain long-term nonrecovery anesthesia in Sprague-Dawley rats. | 2005 Jun |
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Perioperative normothermia depends on intraoperative warming procedure, extent of the surgical intervention and age of the experimental animal. | 2005 Nov 4 |
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Acute aortic rupture in a dog with spirocercosis following the administration of medetomidine. | 2005 Sep |
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Radiosensitising effect of electrochemotherapy with bleomycin in LPB sarcoma cells and tumors in mice. | 2005 Sep 16 |
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Training-induced plasticity of auditory localization in adult mammals. | 2006 Apr |
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Light stimulus frequency dependence of activity in the rat visual system as studied with high-resolution BOLD fMRI. | 2006 May |
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A cardiovascular monitoring system used in conscious cynomolgus monkeys for regulatory safety pharmacology. Part 2: Pharmacological validation. | 2007 Sep-Oct |
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IFN-lambda (IFN-lambda) is expressed in a tissue-dependent fashion and primarily acts on epithelial cells in vivo. | 2008 Mar 14 |
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Late treatment with imatinib mesylate ameliorates radiation-induced lung fibrosis in a mouse model. | 2009 Dec 21 |
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Seizures during medetomindine sedation and local anaesthesia in two dogs undergoing skin biopsy. | 2009 May |
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The non-lemniscal auditory cortex in ferrets: convergence of corticotectal inputs in the superior colliculus. | 2010 |
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Melody, an ENU mutation in Caspase 3, alters the catalytic cysteine residue and causes sensorineural hearing loss in mice. | 2010 Dec |
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Manufacturing and in vivo inner ear visualization of MRI traceable liposome nanoparticles encapsulating gadolinium. | 2010 Dec 18 |
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New class of monoclonal antibodies against severe influenza: prophylactic and therapeutic efficacy in ferrets. | 2010 Feb 8 |
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Cancer treatment dosing regimens of zoledronic acid result in near-complete suppression of mandible intracortical bone remodeling in beagle dogs. | 2010 Jan |
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Sympathetic alpha(2)-adrenoceptors prevent cardiac hypertrophy and fibrosis in mice at baseline but not after chronic pressure overload. | 2010 Jun 1 |
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Microscopic mammalian retinal pigment epithelium lesions induce widespread proliferation with differences in magnitude between center and periphery. | 2010 Mar 31 |
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Physiology and mRNA expression in rainbow trout (Oncorhynchus mykiss) after long-term exposure to the new antifoulant medetomidine. | 2011 Sep |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: http://www.ekavet.com/veterinary-medications/425-domitor-1-mg-ml-solution-for-injection
Curator's Comment: Intended for injection by intramuscular, intravenous and subcutaneous routes in the dog, and by the intramuscular or subcutaneous route in the cat.
for animals:
Dog: 10-30 µg/kg Slight sedation; 30-80 µg/kg Moderate to deep sedation and analgesia; 10-20 µg/kg Pre-anaesthesia
Cat: 50-100 µg/kg Moderate sedation; 100-150 µg/kg Deep sedation;
Route of Administration:
Other
In Vitro Use Guide
Sources: http://www.ncbi.nlm.nih.gov/pubmed/10556684
Rat pineal glands were incubated in oxygenated Krebs-Ringer solution in perifusion chambers, and perifused for 30 min with alpha(2)-adrenoceptor ligands. The melatonin concentrations were measured from the perifusate by radioimmunoassay. Medetomidine (>/=10(-5) M) increased melatonin release.
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NCI_THESAURUS |
C29709
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CFR |
21 CFR 522.1335
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m7128
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BH210P244U
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Z-59
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CHEMBL77921
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C81368
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68601
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86347-15-1
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29428
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300000023831
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ACTIVE MOIETY
SUBSTANCE RECORD