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 |
|---|---|---|
| Promoting effects of xylazine on development of thyroid tumors in rats initiated with N-bis(2-hydroxypropyl)nitrosamine and the mechanism of action. | 2001 Apr |
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| The effect of hepatic microsomal cytochrome P450 monooxygenases on monensin-sulfadimidine interactions in broilers. | 2001 Feb |
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| Results of cystometry and urethral pressure profilometry in dogs sedated with medetomidine or xylazine. | 2001 Feb |
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| Morphometric analysis of early regeneration of motor axons through motor and cutaneous nerve grafts. | 2001 Jul |
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| A novel anaesthetic regimen for surgical procedures in guineapigs. | 2001 Jul |
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| Effects of anesthesia on cystometry and leak point pressure of the female rat. | 2001 Jul 27 |
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| Prejunctional actions of methylenedioxymethamphetamine in vas deferens from wild-type and alpha(2A/D)-adrenoceptor knockout mice. | 2001 Jul 6 |
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| The reversal of xylazine hydrochloride by yohimbine and 4-aminopyridine in goats. | 2001 Jun |
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| [Anesthesia of the New Zealand rabbit using the the combination of tiletamine-zolazepam and ketamine-midazolam with or without xylazine]. | 2001 Jun |
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| Minimal alveolar concentration of desflurane in combination with an infusion of medetomidine for the anaesthesia of ponies. | 2001 Mar 3 |
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| Interaction of formamidine pesticides with the presynaptic alpha(2)-adrenoceptor regulating. | 2001 May 1 |
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| Induction of proteinuric chronic glomerular disease in the rat (Rattus norvegicus) by intracardiac injection of doxorubicin hydrochloride. | 2001 Sep |
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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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| Semen collection from mice: electroejaculation. | 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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| Anesthesia affects the disposition of [18F]fluoro-A-85380: a PET study in monkeys. | 2002 Apr |
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| Measurements of tumor tissue oxygen tension using a time-resolved luminescence-based optical oxylite probe: comparison with a paired survival assay. | 2002 Aug |
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| Xylazine-induced attenuation of dorsal displacement of the soft palate associated with epiglottic dysfunction in a horse. | 2002 Aug 1 |
|
| Effects of treatment with oxytocin, xylazine butorphanol, guaifenesin, acepromazine, and detomidine on esophageal manometric pressure in conscious horses. | 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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| Colonoscopy in mice. | 2002 Jan |
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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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| Cardiovascular phenotypes of kinin B2 receptor- and tissue kallikrein-deficient mice. | 2002 Jul |
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| Use of azaperone and zuclopenthixol acetate to facilitate translocation of white-tailed deer (Odocoileus virginianus). | 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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| Use of the anesthetic combination of tiletamine, zolazepam, ketamine, and xylazine for neutering feral cats. | 2002 May 15 |
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| Arthroscopic removal of dorsoproximal chip fractures of the proximal phalanx in standing horses. | 2002 May-Jun |
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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 |
|
| Enhancement of alpha-adrenoceptor-mediated responses in prostate of testosterone-treated rat. | 2002 Oct 25 |
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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C29709
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ACTIVE MOIETY
SUBSTANCE RECORD
