Levomedetomidine (hydrochloride)
(Synonyms: 盐酸左美托咪定) 目录号 : GC49517
The levorotary enantiomer of medetomidine
Cas No.:190000-46-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Levomedetomidine is the levorotary enantiomer of the racemic α2-adrenergic receptor (α2-AR) agonist medetomidine.1 Unlike medetomidine or the dextrorotary enantiomer dexmedetomidine , levomedetomidine does not induce sedation or analgesia when administered alone in dogs.2 However, levomedetomidine does reduce the level of dexmedetomidine-induced sedation in dogs. Formulations containing levomedetomidine have been used as anesthetics.
1.Kim, S.M., Lee, B., An, H.J., et al.Novel PPARα agonist MHY553 alleviates hepatic steatosis by increasing fatty acid oxidation and decreasing inflammation during agingOncotarget8(28)46273-46285(2017) 2.Kuusela, E., Vainio, O., Kaistinen, A., et al.Sedative, analgesic, and cardiovascular effects of levomedetomidine alone and in combination with dexmedetomidine in dogsAm. J. Vet. Res.62(4)616-621(2001)
| Cas No. | 190000-46-5 | SDF | Download SDF |
| 别名 | 盐酸左美托咪定 | ||
| Canonical SMILES | C[C@@H](C1=CN=CN1)C2=C(C(C)=CC=C2)C.Cl | ||
| 分子式 | C13H16N2 • HCl | 分子量 | 236.7 |
| 溶解度 | DMF: 20 mg/ml,DMSO: 10 mg/ml,Ethanol: 10 mg/ml,PBS (pH 7.2): 1 mg/ml | 储存条件 | -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.2248 mL | 21.1238 mL | 42.2476 mL |
| 5 mM | 0.845 mL | 4.2248 mL | 8.4495 mL |
| 10 mM | 0.4225 mL | 2.1124 mL | 4.2248 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Peripheral α2-adrenoceptor antagonism affects the absorption of intramuscularly coadministered drugs
Vet Anaesth Analg 2018 Jul;45(4):405-413.PMID:29891212DOI:10.1016/j.vaa.2018.01.008.
Objective: We determined the possible effects of a peripherally acting α2-adrenoceptor antagonist, MK-467, on the absorption of intramuscularly (IM) coadministered medetomidine, butorphanol and midazolam. Study design: Randomized, experimental, blinded crossover study. Animals: Six healthy Beagle dogs. Methods: Two IM treatments were administered: 1) medetomidine hydrochloride (20 μg kg-1) + butorphanol (100 μg kg-1) + midazolam (200 μg kg-1; MBM) and 2) MBM + MK-467 hydrochloride (500 μg kg-1; MBM-MK), mixed in a syringe. Heart rate was recorded at regular intervals. Sedation was assessed with visual analog scales (0-100 mm). Drug concentrations in plasma were analyzed with liquid chromatography-tandem mass spectrometry, with chiral separation of dex- and Levomedetomidine. Maximum drug concentrations in plasma (Cmax) and time to Cmax (Tmax) were determined. Paired t-tests, with Bonferroni correction when appropriate, were used for comparisons between the treatments. Results: Data from five dogs were analyzed. Heart rate was significantly higher from 20 to 90 minutes after MBM-MK. The Tmax values for midazolam and Levomedetomidine (mean ± standard deviation) were approximately halved with coadministration of MK-467, from 23 ± 9 to 11 ± 6 minutes (p = 0.049) for midazolam and from 32 ± 15 to 18 ± 6 minutes for Levomedetomidine (p = 0.036), respectively. Conclusions and clinical relevance: MK-467 accelerated the absorption of IM coadministered drugs. This is clinically relevant as it may hasten the onset of peak sedative effects.
Towards scheduled pre-parturient caesarean sections in bitches
Reprod Domest Anim 2020 Jul;55 Suppl 2:38-48.PMID:32374484DOI:10.1111/rda.13669.
Elective caesarean section (CS) is the safest means of delivering the litter in bitches in specific situations. Timeously performing elective pre-parturient CSs at a fixed time would be convenient and prevent emergency CSs and foetal demise. This review proposes a method of performing elective pre-parturient CSs which is safe for both the bitch and puppies. Brachycephaly, small litters and large litters, preceding litter delivered by CS and trial of labour after a preceding CS are identified as factors increasing the need for CS whereas emergency CS is identified as factor increasing foetal demise. The first day of cytological dioestrus more precisely predicts the day of onset of spontaneous parturition than the first day of the LH surge or the dates during oestrus on which progesterone (P4) first exceeds 6 nM or 16 nM. Foetal biparietal diameter at the time of onset of spontaneous parturition varies too much to accurately predict readiness for CS. During the last few days of gestation, P4 with cut-off concentrations at 15.8, 8.7 and 3.18 nM, but not plasma cortisol concentrations, hold promise as predictors of onset of parturition and when to perform pre-parturient CSs. A protocol associating medetomidine hydrochloride as premedicant with propofol as induction agent and sevoflurane as maintenance is safe for scheduled CS and yields good maternal and puppy survival rates at delivery, 2 hr and 7 days after CSs. Clinicians have to pay attention to the haematocrit of bitches at the time of cervical dilatation which is at the lower end of the normal reference ranges for non-pregnant dogs and to the decline in haematocrit during CS (as a proxy for blood loss) which is approximately 7% for both parturient (open cervix) and pre-parturient (closed cervix) CSs. Pre-parturient CSs can be scheduled and performed 57 days after onset of cytological dioestrus with puppy survival rates of 99%. Collectively, these studies provide a protocol to safely perform elective CSs in a large proportion of the obstetric population at a convenient time of the day but more research is required with larger numbers to establish whether this practice is routinely safe and safe in all breeds.
Sedative and cardiopulmonary effects of medetomidine hydrochloride and xylazine hydrochloride and their reversal with atipamezole hydrochloride in calves
Am J Vet Res 2008 Mar;69(3):319-29.PMID:18312129DOI:10.2460/ajvr.69.3.319.
Objective: To assess the sedative and cardiopulmonary effects of medetomidine and xylazine and their reversal with atipamezole in calves. Animals: 25 calves. Procedures: A 2-phase (7-day interval) study was performed. Sedative characteristics (phase I) and cardiopulmonary effects (phase II) of medetomidine hydrochloride and xylazine hydrochloride administration followed by atipamezole hydrochloride administration were evaluated. In both phases, calves were randomly allocated to receive 1 of 4 treatments IV: medetomidine (0.03 mg/kg) followed by atipamezole (0.1 mg/kg; n = 6), xylazine (0.3 mg/kg) followed by atipamezole (0.04 mg/kg; 7), medetomidine (0.03 mg/kg) followed by saline (0.9% NaCl; 6) solution (10 mL), and xylazine (0.3 mg/kg) followed by saline solution (10 mL; 6). Atipamezole or saline solution was administered 20 minutes after the first injection. Cardiopulmonary variables were recorded at intervals for 35 minutes after medetomidine or xylazine administration. Results: At the doses evaluated, xylazine and medetomidine induced a similar degree of sedation in calves; however, the duration of medetomidine-associated sedation was longer. Compared with pretreatment values, heart rate, cardiac index, and PaO(2) decreased, whereas central venous pressure, PaCO(2), and pulmonary artery pressures increased with medetomidine or xylazine. Systemic arterial blood pressures and vascular resistance increased with medetomidine and decreased with xylazine. Atipamezole reversed the sedative and most of the cardiopulmonary effects of both drugs. Conclusions and clinical relevance: At these doses, xylazine and medetomidine induced similar degrees of sedation and cardiopulmonary depression in calves, although medetomidine administration resulted in increases in systemic arterial blood pressures. Atipamezole effectively reversed medetomidine- and xylazine-associated sedative and cardiopulmonary effects in calves.
Echocardiographic assessment of intravenous administration of medetomidine and xylazine hydrochloride at different sedative doses in one-humped camel calves ( Camelus dromedarious)
Vet Res Forum 2022 Mar;13(1):39-46.PMID:35601775DOI:10.30466/vrf.2019.112347.2675.
Echocardiography illustrates a convenient and noninvasive tool for measuring cardiac output (CO) changes after administration of sedative drugs, but it is unknown in camelids practice. The aim of present study was to investigate echocardiographic effects of intravenous (IV) injection of medetomidine and xylazine in camel calves. Twenty apparently healthy immature male one-humped camel calves (Camelus dromedarious) were divided into four groups (five animals in each treatment). Medetomidine and xylazine were injected into the left jugular vein at two different doses of 10.00 and 20.00 μg kg-1 and 0.20 and 0.40 mg kg-1, respectively. Effects on some selected echocardiographic parameters were recorded at different intervals, before drug administrations (baseline) and after 3, 60 and 120 min. Data were analyzed by repeated measure, ANOVA test, then relevance and significance were taken as p ≤ 0.05. Significant decrease in fractional shortening percentage (FS%), ejection fraction percentage (EF%), stroke volume (SV), heart rate (HR) and subsequent CO were noticeable 3 min after drug administration in medetomidine high dose (MH), medetomidine low dose (ML) and xylazine high dose (XH) groups (p ≤ 0.05), furthermore at this time significant decrease in left ventricular mass (LVmass) and left ventricular systolic time intervals were seen in these groups, however, in xylazine low dose (XL) group, the lowest level of most echocardiographic parameters were detectable after 60 min. High dose IV injection of medetomidine was associated with significant decrease in most echocardiographic parameters without echocardiographic arrhythmia. Although, ML and XH groups had the same effects on echocardiographic indices but the intensity and duration were less than MH group.
Differences in the Effects of Pentobarbital Anesthetic and Combination of Medetomidine hydrochloride, Midazolam, and Butorphanol Tartrate Anesthetic on Electroretinogram in Spontaneously Diabetic Torii Fatty Rats
Biomed Hub 2022 Sep 9;7(3):106-114.PMID:36262406DOI:10.1159/000526189.
Purpose: The aim of this study was to investigate the effects of different anesthetic agents on electroretinograms (ERGs) in Spontaneously Diabetic Torii fatty rats (SDT fatty rats). Methods: The ERG recordings were measured under general anesthesia using pentobarbital or a combination of medetomidine hydrochloride, midazolam, and butorphanol (MMB) tartrate anesthesia in 12 9-week-old normal Sprague-Dawley rats (Jcl:SD rats) and 16 SDT fatty rats. Each animal model was divided into 2 groups, the pentobarbital group and MMB group. The amplitudes and peak times of the a- and b-waves and oscillatory potentials (OPs) were measured from 0.0001 candela per square meter (cd.s/m2) to 10.0 cd.s/m2. Results: The amplitude of the a-wave was significantly higher in the MMB group of Jcl:SD rats, but there was no significant difference in amplitude between the two groups of SDT fatty rats. There was no significant difference in the OP1 amplitude between both groups of Jcl:SD rats, but the OP1 amplitude was significantly higher in the MMB group of SDT fatty rats. The OP2 amplitude was significantly higher in the pentobarbital group in both the Jcl:SD rats and SDT fatty rats. There was no significant difference in the OP3 amplitude between the Jcl:SD and SDT fatty rat groups. The amplitude of the OP4 waves was significantly higher in the MMB group for both Jcl:SD and SDT fatty rats. There was no significant difference in the sums of the OP1 to OP4 (ΣOPs) amplitudes between the Jcl:SD and SDT fatty rat groups. There was no significant difference in the b-wave amplitude between the Jcl:SD rat groups, but the b-wave amplitude was significantly higher in the SDT fatty rats that received pentobarbital. The peak times for a-wave, OP1, OP2, OP3, OP4, and ΣOPs were significantly longer in the pentobarbital group of SD rats. The peak time of the b-wave was significantly longer in the MMB group of Jcl:SD rats, but the same result was obtained in the SDT fatty rats except that there was no significant difference in the a-wave. Conclusion: The overall ERG results vary depending on the anesthetic agent used. The OPs can be observed in detail when using MMB. Since the SDT fatty rat is a diabetic model animal, we recommend MMB as the anesthesia of choice when studying the OP waves in detail.