Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C12H16N2S.ClH |
| Molecular Weight | 256.795 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CC1=CC=CC(C)=C1NC2=NCCCS2
InChI
InChIKey=QYEFBJRXKKSABU-UHFFFAOYSA-N
InChI=1S/C12H16N2S.ClH/c1-9-5-3-6-10(2)11(9)14-12-13-7-4-8-15-12;/h3,5-6H,4,7-8H2,1-2H3,(H,13,14);1H
DescriptionCurator's Comment: description was created based on several sources, including:
https://www.ncbi.nlm.nih.gov/pubmed/3062194 | http://www.ema.europa.eu/docs/en_GB/document_library/Maximum_Residue_Limits_-_Report/2009/11/WC500015345.pdf | https://www.drugs.com/vet/rompun-xylazine-100-mg-ml-injectable.html
Curator's Comment: description was created based on several sources, including:
https://www.ncbi.nlm.nih.gov/pubmed/3062194 | http://www.ema.europa.eu/docs/en_GB/document_library/Maximum_Residue_Limits_-_Report/2009/11/WC500015345.pdf | https://www.drugs.com/vet/rompun-xylazine-100-mg-ml-injectable.html
Xylazine was developed as an antihypertensive agent. During clinical studies in people xylazine was found to have excessive central nervous system depressant effects and it was subsequently introduced for veterinary use as a sedative, analgesic and relaxant. Xylazine is a potent alpha-2 adrenergic agonist. Xylazine in horses and Cervidae may occasionally cause slight muscle tremors, bradycardia with partial A-V heart block and a reduced respiratory rate. Movement in response to sharp auditory stimuli may be observed.
CNS Activity
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL3602 |
9.5 µM [IC50] | ||
Target ID: CHEMBL270 |
9.0 µM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Rompun Approved UseRompun™ (xylazine) should be used in horses and Cervidae when it is desirable to produce a state of sedation accompanied by a shorter period of analgesia. Launch Date1995 |
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| Primary | Rompun Approved UseRompun™ (xylazine) should be used in horses and Cervidae when it is desirable to produce a state of sedation accompanied by a shorter period of analgesia. Launch Date1995 |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Long term in-vivo studies of a photo-oxidized bovine osteochondral transplant in sheep. | 2001 |
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| Intraocular pressure in genetically distinct mice: an update and strain survey. | 2001 |
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| Effects of P5, a novel oxazolo(3,2-a)pyridine derivative with a long-acting antihypertensive activity, on different agonist-mediated pressor responses in pithed rats. | 2001 Apr |
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| Severe intoxication from xylazine inhalation. | 2001 Dec |
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| Oral imipramine and intravenous xylazine for pharmacologically-induced ex copula ejaculation in stallions. | 2001 Dec 3 |
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| Morphometric analysis of early regeneration of motor axons through motor and cutaneous nerve grafts. | 2001 Jul |
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| MR imaging-histopathologic correlation of radiofrequency thermal ablation lesion in a rabbit liver model: observation during acute and chronic stages. | 2001 Jul-Sep |
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| Port-site recurrence reproduced in the VX-2 rabbit carcinoma model: an in vivo model comparing laparoscopic port sites and open incisions. | 2001 Jul-Sep |
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| The reversal of xylazine hydrochloride by yohimbine and 4-aminopyridine in goats. | 2001 Jun |
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| Treatment of hypoxemia during xylazine-tiletamine-zolazepam immobilization of wapiti. | 2001 Nov |
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| Corneal toxicity of xylazine and clonidine, in combination with ketamine, in the rat. | 2001 Nov-Dec |
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| Anesthesia protocol for hyperpnea-induced airway obstruction in the guinea pig. | 2001 Oct |
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| Optimization of intraperitoneal injection anesthesia in mice: drugs, dosages, adverse effects, and anesthesia depth. | 2001 Oct |
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| Differences in normal values for murine white blood cell counts and other hematological parameters based on sampling site. | 2001 Oct |
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| Existence of alpha(1A)- and alpha(1B)-adrenoceptor subtypes in canine mandibular alveolar arteries. | 2001 Sep |
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| The effects of ketamine-xylazine anesthesia on cerebral blood flow and oxygenation observed using nuclear magnetic resonance perfusion imaging and electron paramagnetic resonance oximetry. | 2001 Sep 21 |
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| Changes in the acoustically evoked activity in the inferior colliculus of the rat after functional ablation of the auditory cortex. | 2002 |
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| Adaptations to iron deficiency: cardiac functional responsiveness to norepinephrine, arterial remodeling, and the effect of beta-blockade on cardiac hypertrophy. | 2002 |
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| Effects of propofol as an anaesthetic agent in adult lions (Panthera leo): a comparison with two established protocols. | 2002 Apr |
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| Respiratory mechanics in mice: strain and sex specific differences. | 2002 Apr |
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| Anesthesia affects the disposition of [18F]fluoro-A-85380: a PET study in monkeys. | 2002 Apr |
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| The induction of hyperthermia in rabbit liver by means of duplex stainless steel thermoseeds. | 2002 Apr-Jun |
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| Evaluation of anesthesia effects in a rat animal model using otoacoustic emission protocols. | 2002 Aug |
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| Effects of treatment with oxytocin, xylazine butorphanol, guaifenesin, acepromazine, and detomidine on esophageal manometric pressure in conscious horses. | 2002 Dec |
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| In vitro effects of oxytocin, acepromazine, detomidine, xylazine, butorphanol, terbutaline, isoproterenol, and dantrolene on smooth and skeletal muscles of the equine esophagus. | 2002 Dec |
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| Central sympathetic blockade ameliorates brain death-induced cardiotoxicity and associated changes in myocardial gene expression. | 2002 Dec |
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| Male and female rats express similar blood pressure responses to "push-pull" gravitational stress. | 2002 Dec |
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| Effects of Anethum graveolens L. seed extracts on experimental gastric irritation models in mice. | 2002 Dec 19 |
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| Early effects of tribromoethanol, ketamine/xylazine, pentobarbitol, and isoflurane anesthesia on hepatic and lymphoid tissue in ICR mice. | 2002 Feb |
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| Spatial buffering during slow and paroxysmal sleep oscillations in cortical networks of glial cells in vivo. | 2002 Feb 1 |
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| Colonoscopy in mice. | 2002 Jan |
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| Neurohormonal and metabolic effects of medetomidine compared with xylazine in beagle dogs. | 2002 Jan |
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| Assessing the emetic potential of PDE4 inhibitors in rats. | 2002 Jan |
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| The effects of xylazine, detomidine, acepromazine and butorphanol on equine solid phase gastric emptying rate. | 2002 Jul |
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| Murine models of chronic Pseudomonas aeruginosa lung infection. | 2002 Jul |
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| Differential effects of anesthetics on mitochondrial K(ATP) channel activity and cardiomyocyte protection. | 2002 Jul |
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| Effect of general anesthesia and minor surgical trauma on urine and serum measurements in horses. | 2002 Jul |
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| Effects of ketamine-xylazine and isoflurane on insulin sensitivity in dehydroepiandrosterone sulfate-treated minipigs (Sus scrofa domestica). | 2002 Jun |
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| Impact of anesthesia on cardiac function during echocardiography in mice. | 2002 Jun |
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| Periodate-treated, non-anticoagulant heparin-carrying polystyrene (NAC-HCPS) affects angiogenesis and inhibits subcutaneous induced tumour growth and metastasis to the lung. | 2002 Jun 5 |
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| [Castration of male lambs and calves: explanations and comments of art. 65 TSchV]. | 2002 Mar |
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| Modulation of contraction by alpha(2A/D)-adrenoceptors in mouse aorta: evidence employing knockout technology. | 2002 Mar |
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| Thiram inhibits angiogenesis and slows the development of experimental tumours in mice. | 2002 Mar 4 |
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| Use of the anesthetic combination of tiletamine, zolazepam, ketamine, and xylazine for neutering feral cats. | 2002 May 15 |
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| Orthogonal polarisation spectral imaging as a new tool for the assessment of antivascular tumour treatment in vivo: a validation study. | 2002 May 20 |
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| Changes in hepatic and renal enzyme concentrations and heart and respiratory rates in new zealand white rabbits after anesthetic treatments. | 2002 Nov |
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| Infusion of guaifenesin, ketamine, and medetomidine in combination with inhalation of sevoflurane versus inhalation of sevoflurane alone for anesthesia of horses. | 2002 Oct 15 |
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| Rapid degradation of dominant-negative Rab27 proteins in vivo precludes their use in transgenic mouse models. | 2002 Oct 28 |
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| The scotopic threshold response of the dark-adapted electroretinogram of the mouse. | 2002 Sep 15 |
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| A comparison of balloon injury models of endovascular lesions in rat arteries. | 2002 Sep 27 |
Patents
Sample Use Guides
Horse Dosage:
Intravenously–0.5 mL/100 lbs body weight (0.5 mg/lb)
Intramuscularly–1.0 mL/100 lbs body weight (1.0 mg/lb)
Route of Administration:
Other
GLP-compliant studies on mutagenicity included Salmonella-microsomal assay with and without metabolic activation (0.4 to 12 mg of Xylazine on plate, with and without metabolic activation), mammalian forward point mutation assay (HPRT locus) in Chinese hamster lung cells (V79) (2 to 40 ug of Xylazine per ml, with metabolic activation and 62 to 1250 ug of Xylazine per ml, without metabolic activation). The compound to be devoid of mutagenic potential.
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NCI_THESAURUS |
C29709
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m11547
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ACTIVE MOIETY
SUBSTANCE RECORD
