Prolintane (hydrochloride)
(Synonyms: NSC 169914; SP 732) 目录号 : GC44695An Analytical Reference Material
Cas No.:1211-28-5
Sample solution is provided at 25 µL, 10mM.
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- Purity: >98.00%
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Prolintane (hydrochloride) is an analytical reference material that is structurally classified as an amphetamine. It produces stimulant activity by inhibiting transporters for certain monoamine neurotransmitters, including dopamine and norepinephrine, preventing their uptake.[1] Reports of its abuse have been documented.[2] This product is intended for research and forensic applications.
Reference:
[1]. Nicholson, A.N., and Stone, B.M. Heterocyclic amphetamine derivatives and caffeine on sleep in man. Br. J. Clin. Pharmacol. 9(2), 195-203 (1980).
[2]. Kyle, P.B., and Daley, W.P. Domestic abuse of the European rave drug prolintane. J. Anal. Toxicol. 31(7), 415-418 (2007).
Cas No. | 1211-28-5 | SDF | |
别名 | NSC 169914; SP 732 | ||
化学名 | 1-[1-(phenylmethyl)butyl]-pyrrolidine, monohydrochloride | ||
Canonical SMILES | CCCC(N1CCCC1)CC2=CC=CC=C2.Cl | ||
分子式 | C15H23N•HCl | 分子量 | 253.8 |
溶解度 | N/A | 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。 |
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1 mg | 5 mg | 10 mg | |
1 mM | 3.9401 mL | 19.7006 mL | 39.4011 mL |
5 mM | 0.788 mL | 3.9401 mL | 7.8802 mL |
10 mM | 0.394 mL | 1.9701 mL | 3.9401 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 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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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。
The abuse potential of Prolintane in rodents: Behavioral pharmacology approaches
Neuropharmacology 2022 Mar 1;205:108917.PMID:34896117DOI:10.1016/j.neuropharm.2021.108917.
Prolintane (1-Phenyl-2-pyrrolidinylpentane), a synthetic central nervous system (CNS) stimulant, is structurally similar to amphetamine but pharmacologically acts as a dopamine reuptake inhibitor like cocaine. While several case studies reported adverse effects and recreational use of Prolintane, the abuse potential of the drug has not been systemically examined yet. In the present study, we evaluated the behavioral effects of Prolintane regarding its abuse liability in rodents using locomotor activity, conditioned place preference (CPP), self-administration (SA), and drug discrimination paradigms, as well as in-vivo microdialysis experiment. First, acute Prolintane (10 and 20 mg/kg, intraperitoneal injection) increased locomotor activity (distance traveled, cm) in mice but to a lesser degree than methamphetamine (as a positive control). We also found that a single and solitary injection of Prolintane (20 mg/kg, IP) significantly increased extracellular dopamine in the striatum. The following result suggests that its stimulatory effects might be associated with the mesolimbic dopaminergic pathway. Further, Prolintane produced a significant drug-paired place preference at doses of both 10 and 20 mg/kg. In the SA experiment, the mice that self-administered Prolintane intravenously (4 mg/kg/inf) showed a higher infusion and active lever responses but not inactive lever responses. Additionally, cumulative doses of Prolintane partially elicited cocaine-appropriate lever responses (38.57% at doses up to 10 mg/kg) in rats. These results implied that Prolintane has not only rewarding and reinforcing effects but also interoceptive stimulus properties, which are similar to cocaine at a moderate level. Taken together, this study was the first to show, to our knowledge, that Prolintane has a certain level of abuse potential and should be considered carefully as a valuable basis for legal restrictions on use.
Domestic abuse of the European rave drug Prolintane
J Anal Toxicol 2007 Sep;31(7):415-8.PMID:17725890DOI:10.1093/jat/31.7.415.
Prolintane is a sympathomimetic amine with pharmacologic properties similar to d-amphetamine. Side effects include insomnia, nervousness, and irritability. Overdoses of Prolintane may cause hallucinations, psychosis, and death. The drug is commonly prescribed in Africa, Australia, and Europe but is not available in the United States. This manuscript reports the first medically documented cases of Prolintane abuse in the United States. In the first, a 34-year-old male presented to the emergency department confused, agitated, and unable to follow commands. Initial drug and alcohol screens were negative, but analysis by gas chromatography-mass spectrometry (GC-MS) indicated the presence of amitriptyline, nortriptyline, nicotine, and Prolintane. The second patient, a healthy 26-year-old female, presented to the emergency department after intrauterine fetal death and spontaneous delivery. GC-MS revealed the presence of multiple drugs, including cannabinoids, cocaine, nicotine, hydrocodone, and Prolintane. The medical and scientific communities should be aware of the potential for Prolintane abuse because it may cause symptoms similar to those of the amphetamines but is not likely to be detected by a routine urine drug screen.
Study on the metabolism of racemic Prolintane and its optically pure enantiomers
Xenobiotica 1992 Feb;22(2):143-52.PMID:1632104DOI:10.3109/00498259209046613.
1. Asian and European volunteers were given racemic Prolintane, and the metabolites in the 24 h urine were identified and quantified by g.l.c. mass spectroscopy using synthetic reference compounds. 2. R-(+)- and S-(-)-prolintane were synthesized from optically active phenylalanine. The metabolism of the enantiomers differs mainly in the quantitative amounts of metabolites.
Effects of Prolintane on 3,4-dihydroxyphenylacetic acid concentration in rat brain after spiperone treatment
Pharmacol Biochem Behav 1979 Apr;10(4):561-3.PMID:572552DOI:10.1016/0091-3057(79)90233-8.
Prolintane (1-[alpha-propylphenethyl]-pyrrolidine) but not l-(alpha-methylphenethyl)-pyrrolidine markedly enhanced the increase in 3,4-dihydroxyphenylacetic acid concentration in the brains of rats treated with spiperone, a neuroleptic drug. This action and other properties of Prolintane described in the literature place it in a group of stimulant drugs that includes methylphenidate, cocaine and amfonelic acid with properties that differ from those of amphetamine.
[Synthesis of metabolites and enantiomers of Prolintane]
Arch Pharm (Weinheim) 1992 Jan;325(1):47-52.PMID:1605711DOI:10.1002/ardp.19923250111.
The synthesis of 15 possible metabolites of Prolintane (1) (Katovit) which is used in the treatment of blood pressure disregulations is described. Furthermore, the preparation of the enantiomers of 1 is reported, starting with R-(+)- and S-(-)-phenylalaninol respectively.