AP-237 (hydrochloride)
(Synonyms: 盐酸布桂嗪) 目录号 : GC42822An Analytical Reference Standard
Cas No.:17730-82-4
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
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- SDS (Safety Data Sheet)
- Datasheet
AP-237 (hydrochloride) is an analytical reference standard categorized as an analgesic. This product is intended for research and forensic applications.
Cas No. | 17730-82-4 | SDF | |
别名 | 盐酸布桂嗪 | ||
Canonical SMILES | CCCC(N1CCN(C/C=C/C2=CC=CC=C2)CC1)=O.Cl | ||
分子式 | C17H24N2O•HCl | 分子量 | 308.9 |
溶解度 | DMF: 10 mg/ml,DMSO: 15 mg/ml,Ethanol: 30 mg/ml,PBS (pH 7.2): 10 mg/ml | 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。 |
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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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.2373 mL | 16.1865 mL | 32.3729 mL |
5 mM | 0.6475 mL | 3.2373 mL | 6.4746 mL |
10 mM | 0.3237 mL | 1.6186 mL | 3.2373 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。
Analgesic and tolerance studies with AP-237, a new analgesic
Arch Int Pharmacodyn Ther 1975 Jan;213(1):41-57.PMID:1156018doi
1-n-Butyryl-4-cinnamylpiperazine hydrochloride, AP-237, is a new analgesic that has been reported in both Japan and the United States to have good analgesic activity in animals and is currently undergoing clinical trials. A detailed study of the analgesic and side effect profile of this compound is presented. AP-237 was an effective analgesic in a variety of species by several different routes of administration. Results of studies in an inflamed paw pressure and tail flick test in rats, hot plate and writhing test in mice, tooth pulp test in rabbits and intra-arterial bradykinin test in dogs are reported. AP-237 had a low physical dependence liability in rodents as measured by a mouse jumping test and a lack of withdrawal syndrom. Tolerance and cross tolerance results are reported. AP-237 is compared to morphine and pentazocine in most tests.
General pharmacology of a new analgesic-AP-237
Arch Int Pharmacodyn Ther 1975 Jan;213(1):28-40.PMID:1156016doi
1-n-Butyryl-4-cinnamylpiperazine hydrochloride, AP-237, was studied in a variety of general screening tests. Several routes of administration, including oral, subcutaneous, intraperitoneal, and intra-muscular, were employed. It was compared to morphine and pentazocine in many tests. It was found to be a potent analgesic in rats and mice with better oral efficacy than the reference agents. It did not exhibit anti-inflammatory, antipyretic, or anticonvulsant activity but appeared to have some tranquilizing properties. Its general pharmacology resembles the reference agents morphine and pentazocine, but with several differences.
[Clinical observation of filiform fire needling on moderate and severe pain in advanced cancer]
Zhongguo Zhen Jiu 2020 Jun 12;40(6):601-4.PMID:32538009DOI:10.13703/j.0255-2930.20190531-k0001.
Objective: To evaluate the clinical effect of filiform fire needling on moderate and severe pain in advanced cancer. Methods: A total of 66 patients with moderate and severe pain in advanced cancer were randomly divided into an observation group (34 cases, 4 cases dropped off) and a control group (32 cases, 2 cases dropped off). The two groups were treated with oral analgesics continuously for 4 weeks. The moderate pain patients was given bucinnazine hydrochloride tablets (starting at 30 mg, once every 6 hours, increasing by 30%-50% until the titration volume was reached), and the severe pain patients were given oxycodone hydrochloride sustained-release tablets (starting at 20 mg every 12 hours and increasing by 25%-50% until the titration volume was reached). The observation group was cooperated with filiform fire needling at ashi point, Zusanli (ST 36), Liangqiu (ST 34), Qihai (CV 6), Guanyuan(CV 4), Quchi (LI 11) and Waiguan (TE 5) once every other day for 4 weeks. The changes of numerical rating scales (NRS) scores were observed in both groups before and after treatment, and the amount of analgesics and the incidence of adverse reactions were recorded. The clinical effects in the two groups were evaluated. Results: The effective rate was 90.0% (27/30) in the observation group, which was higher than 66.7% (20/30) in the control group (P<0.05). After treatment, the NRS scores of both groups were lower than those before treatment (P<0.05), and the reducing degree in the observation group was larger than that in the control group (P<0.05). The average dosage of bunarizine hydrochloride tablets and oxycodone hydrochloride sustained release tablets to titration volume in the observation group was less than that in the control group (P<0.05). The incidence of adverse reactions was 23.3% (28/120) in the observation group, which was lower than 44.2% (53/120) in the control group (P<0.05). Conclusion: Filiform fire needling can alleviate pain symptoms of patients with moderate and severe pain in advanced cancer, reduce the amount of analgesics, and decrease the incidence of adverse reactions.
[Effects of tramadol hydrochloride injection in relief of cancer pain]
Zhonghua Zhong Liu Za Zhi 1993 Jul;15(4):303-6.PMID:8174470doi
In a prospective multi-centre study, the pain-relieving effects of Tramadol hydrochloride injection were observed in 98 patients with cancer pain. Tramadol was administered 100 mg intramuscularly p.r.n. for 1-3 days, and then the patients were crossed over to AP-237 injection (a common non-narcotic analgesic in China) or Tramal injection (product of Grunenthal) as control. The results showed that the response rates for Tramadol, Tramal and AP-237 were 82.6%, 81.8% and 62.1%, while the side effects were seen in 31%, 21% and 41%, respectively. In conclusion, the pain-relieving effect of Tramadol is as good as that of Tramal, but superior to AP-237.
Comparison of the use of different analgesics in the course of anesthesia care based on pharmacoeconomics
Pak J Pharm Sci 2018 Sep;31(5(Special)):2241-2247.PMID:30463819doi
Narcotic analgesics play an important role in the treatment of pain. If the drug is not standardized, it is easy to cause tolerance and addiction, so scientific management and rational application is very important. In this article, we analyzed the use of narcotic analgesics in a tertiary hospital in 2015-2017. The results showed that the top 3 drugs in DDDs (defined daily doses) were fentanyl transdermal patch (4.2 mg), fentanyl transdermal patch (8.4 mg) and morphine sulfate sustained-release tablets (30 mg). Because of its strong analgesic activity and dosage form, fentanyl has become one of the first choices for severe and moderate pain in clinical practice. Morphine sulfate sustained-release tablets (30 mg) DDDs ranked third in 2015-2017, and the B/A value was 1.75. At the same time, morphine sulfate sustained-release tablets' DDDs declined in 2017 because of the analgesic advantage of bucinnazine hydrochloride injection in emergency treatment. The dosage of pethidine hydrochloride injection is declining year by year, because its analgesic action time is very short and easy to be addicted to, and the long-term application of its metabolite, normethidine, will accumulate in the body, causing neurotoxic symptoms. The price of oxycodone hydrochloride prolonged-release tablets is relatively high, which limits its use to a certain extent. Therefore, recommend rational use of narcotic analgesics in hospitals.