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
| 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 | C12H16N2S |
| Molecular Weight | 220.334 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
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 |
|||
| 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 |
|---|---|---|
| The changes of vitreous pH values in an acute glaucoma rabbit model. | 2001 Aug |
|
| Oral imipramine and intravenous xylazine for pharmacologically-induced ex copula ejaculation in stallions. | 2001 Dec 3 |
|
| The anti-nociceptive efficacy of low dose intramuscular xylazine in lambs. | 2001 Feb |
|
| Hypotensive infarction of the spinal cord in a rhesus macaque (Macaca mulatta). | 2001 Jan |
|
| Comparison of extradural injections of lignocaine and xylazine in azaperone-sedated pigs. | 2001 Jan |
|
| Morphometric analysis of early regeneration of motor axons through motor and cutaneous nerve grafts. | 2001 Jul |
|
| A novel anaesthetic regimen for surgical procedures in guineapigs. | 2001 Jul |
|
| Recovery from carotid artery catheterization performed under various anesthetics in male, Sprague-Dawley rats. | 2001 Jul |
|
| Activation of alpha(2)-receptors in the rostral ventrolateral medulla evokes natriuresis by a renal nerve mechanism. | 2001 Jul |
|
| Prejunctional actions of methylenedioxymethamphetamine in vas deferens from wild-type and alpha(2A/D)-adrenoceptor knockout mice. | 2001 Jul 6 |
|
| Combined xylazine and ketamine as an analgesic regimen in sheep. | 2001 Mar |
|
| Minimal alveolar concentration of desflurane in combination with an infusion of medetomidine for the anaesthesia of ponies. | 2001 Mar 3 |
|
| Interaction of formamidine pesticides with the presynaptic alpha(2)-adrenoceptor regulating. | 2001 May 1 |
|
| Severe intoxication with the veterinary tranquilizer xylazine in humans. | 2001 May-Jun |
|
| Corneal toxicity of xylazine and clonidine, in combination with ketamine, in the rat. | 2001 Nov-Dec |
|
| Anesthesia protocol for hyperpnea-induced airway obstruction in the guinea pig. | 2001 Oct |
|
| Differences in normal values for murine white blood cell counts and other hematological parameters based on sampling site. | 2001 Oct |
|
| Focal synchronization of ripples (80-200 Hz) in neocortex and their neuronal correlates. | 2001 Oct |
|
| Adaptations to iron deficiency: cardiac functional responsiveness to norepinephrine, arterial remodeling, and the effect of beta-blockade on cardiac hypertrophy. | 2002 |
|
| Anesthesia affects the disposition of [18F]fluoro-A-85380: a PET study in monkeys. | 2002 Apr |
|
| The induction of hyperthermia in rabbit liver by means of duplex stainless steel thermoseeds. | 2002 Apr-Jun |
|
| Evaluation of anesthesia effects in a rat animal model using otoacoustic emission protocols. | 2002 Aug |
|
| Measurements of tumor tissue oxygen tension using a time-resolved luminescence-based optical oxylite probe: comparison with a paired survival assay. | 2002 Aug |
|
| Effects of treatment with oxytocin, xylazine butorphanol, guaifenesin, acepromazine, and detomidine on esophageal manometric pressure in conscious horses. | 2002 Dec |
|
| Similar half-octave TTS protection of the cochlea by xylazine/ketamine or sympathectomy. | 2002 Dec |
|
| Colonoscopy in mice. | 2002 Jan |
|
| The effects of xylazine, detomidine, acepromazine and butorphanol on equine solid phase gastric emptying rate. | 2002 Jul |
|
| Differential effects of anesthetics on mitochondrial K(ATP) channel activity and cardiomyocyte protection. | 2002 Jul |
|
| Investigation of neurotransmission in vas deferens from alpha(2A/D)-adrenoceptor knockout mice. | 2002 Jul |
|
| Effects of ketamine-xylazine and isoflurane on insulin sensitivity in dehydroepiandrosterone sulfate-treated minipigs (Sus scrofa domestica). | 2002 Jun |
|
| The scotopic threshold response of the dark-adapted electroretinogram of the mouse. | 2002 Sep 15 |
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.
| Substance Class |
Chemical
Created
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admin
on
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| Record UNII |
NGC3S0882S
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Validated (UNII)
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C29709
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