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
Molecular Formula | ClH |
Molecular Weight | 36.461 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | C13H16N2 |
Molecular Weight | 200.2795 |
Charge | 0 |
Count |
|
Stereochemistry | RACEMIC |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Optical Activity | ( + / - ) |
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 |
---|---|---|
Effects of anticholinergic treatment on the cardiac and respiratory systems in dogs sedated with medetomidine. | 1991 Oct 5 |
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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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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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Acute aortic rupture in a dog with spirocercosis following the administration of medetomidine. | 2005 Sep |
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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 |
|
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 Dec |
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Degradable gelatin microspheres as an embolic agent: an experimental study in a rabbit renal model. | 2007 Sep-Oct |
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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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Vascular disrupting action of electroporation and electrochemotherapy with bleomycin in murine sarcoma. | 2008 Jan 29 |
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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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EphrinB2 induces tyrosine phosphorylation of NR2B via Src-family kinases during inflammatory hyperalgesia. | 2008 Sep 22 |
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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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Retrograde adenoviral vector targeting of nociresponsive pontospinal noradrenergic neurons in the rat in vivo. | 2009 Jan 10 |
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Seizures during medetomindine sedation and local anaesthesia in two dogs undergoing skin biopsy. | 2009 May |
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Nitric oxide synthase enzymes in the airways of mice exposed to ovalbumin: NOS2 expression is NOS3 dependent. | 2010 |
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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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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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Adaptation to stimulus statistics in the perception and neural representation of auditory space. | 2010 Jun 24 |
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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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Creating a population-averaged standard brain template for Japanese macaques (M. fuscata). | 2010 Oct 1 |
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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.
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 16:06:41 GMT 2023
by
admin
on
Fri Dec 15 16:06:41 GMT 2023
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Record UNII |
BH210P244U
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Record Status |
Validated (UNII)
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Record Version |
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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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Related Record | Type | Details | ||
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PARENT -> SALT/SOLVATE | |||
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ENANTIOMER -> RACEMATE |
Related Record | Type | Details | ||
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ACTIVE MOIETY |