Pirenperone
(Synonyms: R-47456, R-50656) 目录号 : GC25756Pirenperone (R-47456, R-50656), a quinazoline derivative, is a selective antagonist of SR-2A (5-HT2 serotonin receptor) when employed in low doses. Pirenperone behaves like a typical neuroleptic when used in higher doses (greater than 0.1 mg/kg).
Cas No.:75444-65-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Pirenperone (R-47456, R-50656), a quinazoline derivative, is a selective antagonist of SR-2A (5-HT2 serotonin receptor) when employed in low doses. Pirenperone behaves like a typical neuroleptic when used in higher doses (greater than 0.1 mg/kg).
[1] L Paw?owski, et al. Pol J Pharmacol Pharm. Mar-Apr 1985;37(2):179-96.
| Cas No. | 75444-65-4 | SDF | Download SDF |
| 别名 | R-47456, R-50656 | ||
| 分子式 | C23H24FN3O2 | 分子量 | 393.45 |
| 溶解度 | DMSO: 17 mg/mL (43.21 mM);Water: Insoluble;Ethanol: 26 mg/mL (66.08 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。 |
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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 | 2.5416 mL | 12.7081 mL | 25.4162 mL |
| 5 mM | 0.5083 mL | 2.5416 mL | 5.0832 mL |
| 10 mM | 0.2542 mL | 1.2708 mL | 2.5416 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。
Pirenperone relieves the symptoms of fragile X syndrome in Fmr1 knockout mice
Sci Rep 2022 Dec 5;12(1):20966.PMID:36470953DOI:10.1038/s41598-022-25582-8.
Fragile X syndrome (FXS) is a neurodevelopmental disorder that is caused by the loss of Fragile X-linked mental retardation protein (FMRP), an RNA binding protein that can bind and recognize different RNA structures and regulate the target mRNAs' translation involved in neuronal synaptic plasticity. Perturbations of this gene expression network have been related to abnormal behavioral symptoms such as hyperactivity, and impulsivity. Considering the roles of FMRP in the modulation of mRNA translation, we investigated the differentially expressed genes which might be targeted to revert to normal and ameliorate behavioral symptoms. Gene expression data was analyzed and used the connectivity map (CMap) to understand the changes in gene expression in FXS and predict the effective drug candidates. We analyzed the GSE7329 dataset that had 15 control and 8 FXS patients' lymphoblastoid samples. Among 924 genes, 42 genes were selected as signatures for CMap analysis, and 24 associated drugs were found. Pirenperone was selected as a potential drug candidate for FXS for its possible antipsychotic effect. Treatment of Pirenperone increased the expression level of Fmr1 gene. Moreover, Pirenperone rescued the behavioral deficits in Fmr1 KO mice including hyperactivity, spatial memory, and impulsivity. These results suggest that Pirenperone is a new drug candidate for FXS, which should be verified in future studies.
Selective effects of Pirenperone on analgesia produced by morphine or electrical stimulation at sites in the nucleus raphe magnus and periaqueductal gray
Psychopharmacology (Berl) 1986;88(2):172-6.PMID:3081929DOI:10.1007/BF00652235.
Pirenperone, a new serotonin antagonist with a selective affinity for the 5-HT2 receptor, was administered in conjunction with tests for the antinociceptive effects of morphine sulphate and electrical brain-stimulation at sites in the periaqueductal gray (PAG) and nucleus raphe magnus (NRM). Nociception was assessed by tail-flick latencies in a warm water bath and Pirenperone (0.04-0.16 mg/kg) had no effect on baseline scores. When administered prior to morphine, Pirenperone (0.16 mg/kg) caused significant attenuation of analgesia induced by morphine. Comparable effects of Pirenperone were observed when analgesia was produced by electrical stimulation of the NRM. In contrast, Pirenperone had no effect on the analgesic effects of PAG stimulation. This pattern of results suggests that a system involving supraspinal 5-HT2 receptors may modulate some of the antinociceptive effects of morphine and stimulation of the NRM. The differential effects of Pirenperone on stimulation-produced analgesia at sites in the NRM and PAG is consistent with separate neural substrates for the analgesia observed from stimulation of these two brain regions.
Maturational age affects Pirenperone dose-response pattern
Gen Pharmacol 1987;18(3):225-7.PMID:3569849DOI:10.1016/0306-3623(87)90003-6.
The effects of the 5-HT2 antagonist Pirenperone on temperature preference were observed 1 hr after injection in mice aged 3, 5 and 7 days and at doses of 0.16, 0.48 and 1.6 mg/kg body weight. Although all 3 doses produced significant decreases in preferred temperature at 3 days, only the highest dose had significant effects at ages 5 and 7 days. Analysis of the data suggests that the dose-response relationship depends on age in a way that would be consistent with a shift in the dose-response curve with increasing age.
A characterization of LSD-antagonist effects of Pirenperone in the rat
Neuropharmacology 1983 Aug;22(8):1001-5.PMID:6621823DOI:10.1016/0028-3908(83)90216-2.
Rats were trained to discriminate between intraperitoneal injections of 0.16 mg/kg of d-lysergic acid diethylamide (d-LSD) and injections of saline in the two-bar (FR 10) food-reinforced drug discrimination procedure. The gradient for responses to LSD was established following pretreatment with saline or one of five doses of Pirenperone. It was found that pretreatment with Pirenperone caused a parallel shift to the right of the dose-effect curve of LSD. The magnitude of this shift was related to the dose of Pirenperone, 0.006 mg/kg of the drug causing a 2-fold shift. A direct linear plot revealed that the curve fitting the data points passed through the origin, but that it was curvilinear rather than linear. The data did not, therefore, accommodate the requirements for reversible, competitive interaction. This finding is discussed in terms of the mixed agonist/antagonist activity of LSD that may occur at binding sites for 5-HT1 and 5-HT2 in the rat brain.
Central antiserotonergic and antidopaminergic action of Pirenperone, a putative 5-HT2 receptor antagonist
Pol J Pharmacol Pharm 1985 Mar-Apr;37(2):179-96.PMID:4048012doi
Pirenperone, an antagonist of 5-HT2 but not 5-HT1 receptors, has been studied for its central antiserotonergic and antidopaminergic activity. Pirenperone (0.00525-0.1 mg/kg) antagonized dose-dependently stimulation of the hind limb flexor reflex in spinal rats induced by LSD, quipazine or fenfluramine, and hyperthermia induced by serotonin (5-hydroxytryptamine; 5-HT)-like drugs (1-5-hydroxytryptophan, fenfluramine, p-chloroamphetamine, 1-/m-chlorophenyl/-piperazine, quipazine) in heat-adapted rats. Pirenperone also counteracted tryptamine-induced convulsions in rats (ID50 = 0.87 mg/kg); however, this action was weaker than that of metergoline (ID50 = 0.22 mg/kg). Pirenperone (0.1-1.6 mg/kg) produced sedation in mice and rats, and-in doses of 0.4-6.4 mg/kg-catalepsy in rats. Given in doses ranging from 0.1 to 1.6 mg/kg, Pirenperone antagonized d-amphetamine-induced locomotor hyperactivity in mice and rats, the hyperactivity induced by apomorphine in rats, apomorphine- or d-amphetamine-induced stereotypy in rats and stimulation of the hind limb flexor reflex induced by the alpha-adrenoceptor agonist-clonidine. Pirenperone (6.4 mg/kg) significantly attenuated apomorphine (1 mg/kg)-induced hypothermia in mice. The results obtained indicate that Pirenperone may be regarded as a relatively specific antagonist of the 5-HT2 receptor only when it is employed in very low doses (less than 0.1 mg/kg). Used in higher doses (greater than 0.1 mg/kg), it behaves like a typical neuroleptic, i.e. like a dopamine antagonist with antiserotonergic, antitryptaminergic and antiadrenergic properties.