Propionylpromazine hydrochloride
(Synonyms: 盐酸丙酰丙嗪,Propiopromazine hydrochloride) 目录号 : GC39736
A promazine neuroleptic and dopamine receptor antagonist
Cas No.:7681-67-6
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Propionylpromazine is a promazine neuroleptic and dopamine receptor antagonist.1,2,3 It is an antagonist at the I. scapularis (tick) dopamine 2 receptor (Isdop2) and A. aegypti (mosquito) dopamine 2 receptor (AaDOP2), providing 94 and 85% inhibition, respectively, in a chemical screening assay at 10 ?M.4,3 Propionylpromazine inhibits recombinant T. cruzi trypanothione reductase (IC50 = 357 ?M) and is active against T. brucei trypomastigotes (ED50 = 10.1 ?M) but not L. donovani amastigotes or T. cruzi trypomastigotes (ED50s = >30 ?M) in mouse peritoneal macrophages.5 It increases survival of C. elegans in a model of paraquat-induced oxidative stress.6 Propionylpromazine reduces stereotypic behavior induced by apomorphine in rats (ED50 = 2.5 mg/kg, s.c.).1 Formulations containing propionylpromazine have been used as tranquilizers in veterinary medicine.
1.Fielding, S., and Lal, H.Biochemical actions of neuroleptic drugs: focus on the dopamine receptorHandbook of psychopharmacology37-55(1978) 2.Ejendal, K.F.K., Meyer, J.M., Brust, T.F., et al.Discovery of antagonists of tick dopamine receptors via chemical library screening and comparative pharmacological analysesInsect Biochem. Molec.42(11)846-853(2012) 3.Meyer, J.M., Ejendal, K.F.K., Avramova, L.V., et al.A "genome-to-lead" approach for insecticide discovery: pharmacological characterization and screening of Aedes aegypti D(1)-like dopamine receptorsPlos Negl. Trop. D.6(1)e1478(2012) 4.Ejendal, K.F.K., Meyer, J.M., Brust, T.F., et al.Discovery of antagonists of tick dopamine receptors via chemical library screening and comparative pharmacological analysesInsect Biochem. Molec.42(11)846-853(2012) 5.Chan, C., Yin, H., Garforth, J., et al.Phenothiazine inhibitors of trypanothione reductase as potential antitrypanosomal and antileishmanial drugsJ. Med. Chem.41(2)148-156(1998) 6.Ye, X., Linton, J.M., Schork, N.J., et al.A pharmacological network for lifespan extension in Caenorhabditis elegansAging Cell13(2)206-215(2014)
| Cas No. | 7681-67-6 | SDF | |
| 别名 | 盐酸丙酰丙嗪,Propiopromazine hydrochloride | ||
| Canonical SMILES | CCC(C(C=C1N2CCCN(C)C)=CC=C1SC3=C2C=CC=C3)=O.[H]Cl | ||
| 分子式 | C20H25ClN2OS | 分子量 | 376.94 |
| 溶解度 | DMSO: 83.33 mg/mL (221.07 mM) | 储存条件 | Store at -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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.6529 mL | 13.2647 mL | 26.5294 mL |
| 5 mM | 0.5306 mL | 2.6529 mL | 5.3059 mL |
| 10 mM | 0.2653 mL | 1.3265 mL | 2.6529 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。
Stability of the tranquilizer drug Propionylpromazine hydrochloride in formulated products
Pest Manag Sci 2005 Jun;61(6):605-11.PMID:15668921DOI:10.1002/ps.1018.
An analytical method to evaluate Propionylpromazine hydrochloride (PPZHCl) in tranquilizer formulations was developed using high-performance liquid chromatography (HPLC). During analysis of aged quality-control samples, a previously unreported chromatographic response was observed at a shorter retention time than PPZHCl. Further investigation of formulations stored in trap tap devices at temperatures ranging from 5 to 40 degrees C during field trials at four different locations confirmed the degradation of the active ingredient. Further investigation using HPLC/tandem mass spectrometry revealed two to five degradates, with the major degradates being oxidation products of the active ingredient, PPZHCl. As PPZHCl formulations must be stable when stored at 5 to 40 degrees C for 6 to 12 months, reformulation with the anti-oxidant ascorbic acid was utilized to achieve the required PPZHCl stability.
Analysis of propionylpromazine and its metabolites in horse urine
Cornell Vet 1984 Jan;74(1):38-49.PMID:6705538doi
The metabolism of propionylpromazine in the horse was studied. Although propionylpromazine is not currently approved or recommended for use in horses, it has been used illegally to alter their performance. Propionylpromazine hydrochloride was administered intramuscularly at clinical and subclinical doses. Three metabolites were detected in urine. The major metabolite was identified as 2-(1-hydroxypropyl) promazine sulfoxide. The detection of this metabolite in routine drug testing has been described.
Determination of Propionylpromazine hydrochloride in formulation matrixes using reversed-phase ion-pair small bore liquid chromatography
J AOAC Int 1999 Nov-Dec;82(6):1321-8.PMID:10589483doi
Propionylpromazine hydrochloride (PPZHCl) has been investigated for use with leghold traps to reduce the amount of self-inflicted trauma experienced by animals restrained by these traps. Three types of PPZHCl formulations made with Karo dark syrup, K-Y Jelly, and Vaseline were used in 2 types of tranquilizer trap devices (TTDs). A reversed-phase ion-pair liquid chromatography (LC) method using a small bore C18 column was used to: (1) determine the purity of the PPZHCl material used in these formulations, and (2) to determine the resulting PPZHCl content of each formulation. Analyte quantitation was done using UV absorption at 280 nm. Regression analysis of calibration standard solutions indicated a linear and directly proportional relationship between analyte response and PPZHCl concentration over the range evaluated. Recovery data from: (1) Vaseline formulations containing 38.8, 16.2, and 8.78% PPZHCl were 104, 92.9, and 90.2%, respectively, (2) Karo dark syrup formulations containing 26.5, 18.1, and 10.3% PPZHCl were 97.7, 99.3, and 106%, respectively, and (3) K-Y Jelly formulations containing 33.0, 23.5, and 13.4% PPZHCl were 100, 99.4, and 88.7%, respectively. The relative standard deviation (RSD) values from triplicate analysis of these formulations ranged from 0.7 to 6.7%. The PPZHCl content from 9 manufactured TTDs, 3 for each formulation type, were analyzed in triplicate and produced RSD values ranging from 0.7-6.8%. These results indicate that the formulation extraction presented could be used to evaluate the PPZHCl content in TTDs prior to field use. The use of a small bore LC column reduced the amount of solvents consumed and hazardous waste generated, compared to sample analysis that uses a more conventional analytical LC column.
Development of a solid phase extraction method for simultaneous determination of corticoids and tranquilizers in serum samples
J Sep Sci 2004 Jan;27(1-2):53-8.PMID:15335058DOI:10.1002/jssc.200301569.
A simple and fast solid phase extraction (SPE) method allowing the preconcentration, clean-up, and subsequent separate elution of phenothiazines (chlorpromazine hydrochloride, acetopromazine, and Propionylpromazine hydrochloride) and glucocorticoids (dexamethasone, betamethasone acetate, and phenylbutazone) from serum samples has been developed. Both fractions were separately collected and analyzed without any additional treatment by high performance liquid chromatography with UV-Vis. The performance of the complete procedure was satisfactory irrespective of the spiking level with recoveries in the range 64-85% for all analytes investigated but for phenylbutazone (20%). Repeatability, evaluated as the relative standard deviation, was globally better than 12%. LC-MS was used for final confirmation of the results.