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=CC=CC(C)=C2C
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 |
|---|---|---|---|
Target ID: CHEMBL2095158 Sources: http://www.ncbi.nlm.nih.gov/pubmed/2571177 |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| 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 |
|---|---|---|
| Physiology and mRNA expression in rainbow trout (Oncorhynchus mykiss) after long-term exposure to the new antifoulant medetomidine. | 2011-09 |
|
| Manufacturing and in vivo inner ear visualization of MRI traceable liposome nanoparticles encapsulating gadolinium. | 2010-12-18 |
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| Melody, an ENU mutation in Caspase 3, alters the catalytic cysteine residue and causes sensorineural hearing loss in mice. | 2010-12 |
|
| Creating a population-averaged standard brain template for Japanese macaques (M. fuscata). | 2010-10-01 |
|
| Tissue restoration after implantation of polyglycolide, polydioxanone, polylevolactide, and metallic pins in cortical bone: an experimental study in rabbits. | 2010-07 |
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| Adaptation to stimulus statistics in the perception and neural representation of auditory space. | 2010-06-24 |
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| Lysophosphatidylcholine as an adjuvant for lentiviral vector mediated gene transfer to airway epithelium: effect of acyl chain length. | 2010-06-23 |
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| Sympathetic alpha(2)-adrenoceptors prevent cardiac hypertrophy and fibrosis in mice at baseline but not after chronic pressure overload. | 2010-06-01 |
|
| Epidermal neural crest stem cell (EPI-NCSC)--mediated recovery of sensory function in a mouse model of spinal cord injury. | 2010-06 |
|
| Microscopic mammalian retinal pigment epithelium lesions induce widespread proliferation with differences in magnitude between center and periphery. | 2010-03-31 |
|
| New class of monoclonal antibodies against severe influenza: prophylactic and therapeutic efficacy in ferrets. | 2010-02-08 |
|
| Cancer treatment dosing regimens of zoledronic acid result in near-complete suppression of mandible intracortical bone remodeling in beagle dogs. | 2010-01 |
|
| Nitric oxide synthase enzymes in the airways of mice exposed to ovalbumin: NOS2 expression is NOS3 dependent. | 2010 |
|
| The non-lemniscal auditory cortex in ferrets: convergence of corticotectal inputs in the superior colliculus. | 2010 |
|
| Late treatment with imatinib mesylate ameliorates radiation-induced lung fibrosis in a mouse model. | 2009-12-21 |
|
| Seizures during medetomindine sedation and local anaesthesia in two dogs undergoing skin biopsy. | 2009-05 |
|
| Retrograde adenoviral vector targeting of nociresponsive pontospinal noradrenergic neurons in the rat in vivo. | 2009-01-10 |
|
| Serotonin transporter genotype modulates social reward and punishment in rhesus macaques. | 2009 |
|
| The effects of medetomidine hydrochloride on the electroretinogram of normal dogs. | 2008-12-03 |
|
| EphrinB2 induces tyrosine phosphorylation of NR2B via Src-family kinases during inflammatory hyperalgesia. | 2008-09-22 |
|
| IFN-lambda (IFN-lambda) is expressed in a tissue-dependent fashion and primarily acts on epithelial cells in vivo. | 2008-03-14 |
|
| Vascular disrupting action of electroporation and electrochemotherapy with bleomycin in murine sarcoma. | 2008-01-29 |
|
| Estrogen sensitivity of target genes and expression of nuclear receptor co-regulators in rat prostate after pre- and postnatal exposure to the ultraviolet filter 4-methylbenzylidene camphor. | 2007-12 |
|
| Degradable gelatin microspheres as an embolic agent: an experimental study in a rabbit renal model. | 2007-10-10 |
|
| A cardiovascular monitoring system used in conscious cynomolgus monkeys for regulatory safety pharmacology. Part 2: Pharmacological validation. | 2007-02-23 |
|
| Light stimulus frequency dependence of activity in the rat visual system as studied with high-resolution BOLD fMRI. | 2006-05 |
|
| Training-induced plasticity of auditory localization in adult mammals. | 2006-04 |
|
| 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. | 2005-12-15 |
|
| Perioperative normothermia depends on intraoperative warming procedure, extent of the surgical intervention and age of the experimental animal. | 2005-11-04 |
|
| Radiosensitising effect of electrochemotherapy with bleomycin in LPB sarcoma cells and tumors in mice. | 2005-09-16 |
|
| Acute aortic rupture in a dog with spirocercosis following the administration of medetomidine. | 2005-09 |
|
| Evaluation of two combinations of Domitor, Zoletil 100, and Euthatal to obtain long-term nonrecovery anesthesia in Sprague-Dawley rats. | 2005-06 |
|
| [Domitor not to used in collies?]. | 2003-05-15 |
|
| Regulation of Cl- secretion by alpha2-adrenergic receptors in mouse colonic epithelium. | 2003-04-15 |
|
| Reduced blood flow and oxygenation in SA-1 tumours after electrochemotherapy with cisplatin. | 2002-10-21 |
|
| Effects of preemptive atropine administration on incidence of medetomidine-induced bradycardia in dogs. | 2001-01-01 |
|
| Postoperative analgesic and cardiopulmonary effects in dogs of oxymorphone administered epidurally and intramuscularly, and medetomidine administered epidurally: a comparative clinical study. | 1996-07-01 |
|
| Comparison of neurologic responses to the use of medetomidine as a sole agent or preanesthetic in laboratory beagles. | 1992 |
|
| Effects of anticholinergic treatment on the cardiac and respiratory systems in dogs sedated with medetomidine. | 1991-10-05 |
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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29428
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300000023831
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ACTIVE MOIETY
SUBSTANCE RECORD