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Meptazinol HCl
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Meptazinol HCl图片
CAS NO:59263-76-2
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)269.81
FormulaC15H23NO.HCl
CAS No.59263-76-2
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 54 mg/mL (200.1 mM)
Water: 54 mg/mL (200.1 mM)
Ethanol: 54 mg/mL (200.1 mM)
Other info

Chemical Name: 3-(3-Ethylhexahydro-1-methyl-1H-azepin-3-yl)phenol hydrochloride

InChi Key: MPJUSISYVXABBH-UHFFFAOYSA-N

InChi Code: InChI=1S/C15H23NO.ClH/c1-3-15(9-4-5-10-16(2)12-15)13-7-6-8-14(17)11-13;/h6-8,11,17H,3-5,9-10,12H2,1-2H3;1H

SMILES Code: OC1=CC=CC(C2(CC)CN(C)CCCC2)=C1.[H]Cl

Synonyms

IL 22811 HCl; WY 22811; IL-22811; WY-22811; IL22811; WY22811; Meptazinol Hydrochloride, trade name Meptid.

实验参考方法
In Vitro

In vitro activity: Meptazinol inhibits a portion of 3H-labeled opiate and opioid peptide binding quite potently, with IC50 value under 1 nM.

In VivoNaloxonazine treatment 24 hr earlier attenuates Meptazinol (10 mg/kg i.v.) analgesia in both the mouse writhing and rat tail-flick assays. Meptazinol administered with morphine does not reverse the respiratory depressant actions seen with morphine alone, distinguishing meptazinol from other mixed agonist/antagonists. The absorption of Meptazinol (8 mg/kg i.v.) from nasal cavity to systemic circulation is rapid and complete in male Sprague-Dawley rats. The maximum observed concentration is achieved at 15 min after administration and the absolute bioavailability is 96.06%. The cerebrospinal fluid level of Meptazinol (8 mg/kg i.v.) attains a high concentration of 2.71 μg/mL and then is followed by an exponential decline. The concentration of intravenous Meptazinol (8 mg/kg i.v.) achieves a peak at 10 min followed by a steep decline in the cortex dialysate. Inclusion of Meptazinol (2 mg/kg) reduces the total dose of anaesthetic required, allows a more rapid recovery and is associated with less movement in response to surgery in cystoscopy patients. The patients in the control group tends to hyperventilate, and has lower end-tidal CO2 tension, and also higher pulse rates during surgery than the Meptazinol group. Meptazinol (25 mg/kg) evokes larger increases in nociceptive thresholds in the mouse than in the rat, whereas morphine induces large increases in both species. Antinociceptive responses to Meptazinol are consistently inhibited in animals pretreated with naloxone, whereas scopolamine attenuates the effects of meptazinol in some, particularly the mouse tail immersion test. Meptazinol (2 mg/kg i.v.) greatly reduces the incidence of ventricular extrasystoles that resulted from acute coronary artery occlusion as well as ventricular fibrillation (VF) in rats. Meptazinol also reduces ventricular arrhythmias, including fibrillation, in conscious rats subjected to coronary artery occlusion
Animal modelMice
Formulation & Dosage10 mg/kg i.v.
References

J Pharmacol Exp Ther. 1984 Feb;228(2):414-9; Life Sci. 2005 Sep 30;77(20):2574-83; Anaesthesia. 1985 May;40(5):490-3.