Altanserin
(Synonyms: 阿坦色林) 目录号 : GC64387
Altanserin 可用于合成 Fluorine-18 Altanserin。Fluorine-18 Altanserin 可与脑 5HT2 受体结合.
Cas No.:76330-71-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Altanserin can synthesize Fluorine-18 Altanserin. Fluorine-18 Altanserin binds to the brain 5HT2 receptors[1].
Altanserin can synthesize Fluorine-18 Altanserin[1].
[1]. Biver F, et al. Multicompartmental study of fluorine-18 altanserin binding to brain 5HT2 receptors in humans using positron emission tomography. Eur J Nucl Med. 1994;21(9):937-946.
| Cas No. | 76330-71-7 | SDF | Download SDF |
| 别名 | 阿坦色林 | ||
| 分子式 | C22H22FN3O2S | 分子量 | 411.49 |
| 溶解度 | DMSO : 19.23 mg/mL (46.73 mM; ultrasonic and warming and heat to 60°C) | 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 | 2.4302 mL | 12.151 mL | 24.3019 mL |
| 5 mM | 0.486 mL | 2.4302 mL | 4.8604 mL |
| 10 mM | 0.243 mL | 1.2151 mL | 2.4302 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。
Measurement of changes in endogenous serotonin level by positron emission tomography with [18F]Altanserin
Ann Nucl Med 2021 Aug;35(8):955-965.PMID:34101154DOI:10.1007/s12149-021-01633-4.
Objective: Positron emission tomography (PET) has been used to investigate changes in the concentration of endogenous neurotransmitters. Recently, this technique has been applied to the imaging of serotonin2A receptors using [18F]Altanserin. In these measurements, a reduction in binding potential (BP) suggests an increase in endogenous serotonin levels caused by pharmacological or cognitive stimulations, and the sensitivity of BP reduction depends on the characteristics of [18F]Altanserin. In this study, we evaluated an analytical method for estimating the changes in endogenous serotonin levels based on PET scans with [18F]Altanserin at baseline and stimulated states and validated it using simulations and small animal PET studies. Methods: First, in the simulations, the time-activity curves at baseline and the stimulated states were generated using an extended compartment model including the competition for the receptors between the administered [18F]Altanserin and endogenous serotonin. In the stimulated state, the magnitude and onset of the endogenous serotonin elevation were altered to varying degrees. In these time-activity curves, BP was estimated using the simplified reference tissue model (SRTM), and the reduction in BP was evaluated by comparison with that of the baseline state. Next, the proposed method was applied to mouse PET studies. Endogenous serotonin levels were elevated by treatment with selective serotonin reuptake inhibitors (SSRIs), and PET studies were performed twice, once with and once without treatment. In both scans, BP was estimated using the SRTM with the cerebellum as a reference region, and the reduction in BP after SSRI treatment was evaluated. Results: In the simulations, the BP estimate of the stimulated state was smaller than that of the baseline state, and their reduction was related to the amount of change in the serotonin concentration. BP reduction was also affected by the onset of serotonin elevation. In the mouse studies, the BP of the cerebral cortex decreased in the scans with SSRI treatment. Conclusions: The reduction in BP estimated using the SRTM from [18F]altanserin-PET studies at baseline and in stimulated states can detect changes in the binding conditions of serotonin2A receptors. This may be useful for investigating the elevation of endogenous serotonin levels caused by stimulations.
[18F]Altanserin binding to human 5HT2A receptors is unaltered after citalopram and pindolol challenge
J Cereb Blood Flow Metab 2004 Sep;24(9):1037-45.PMID:15356424DOI:10.1097/01.WCB.0000126233.08565.E7.
The aim of the present study was to develop an experimental paradigm for the study of serotonergic neurotransmission in humans using positron emission tomography and the 5-HT2A selective radioligand [18F]Altanserin. [18F]Altanserin studies were conducted in seven subjects using the bolus/infusion approach designed for attaining steady state in blood and brain 2 hours after the initial [18F]Altanserin administration. Three hours after commencement of radiotracer administration, 0.25 mg/kg of the selective serotonin reuptake inhibitor, citalopram (Lundbeck, Valby, Denmark), was administered to all subjects as a constant infusion for 20 minutes. To reduce 5-HT1A-mediated autoinhibition of cortical 5-HT release, four of the seven subjects were pretreated with the partial 5-HT1A agonist pindolol for 3 days at an increasing oral dose (25 mg on the day of scanning). In each subject, the baseline condition (120 to 180 minutes) was compared with the stimulated condition (195 to 300 minutes). Despite a pronounced increase in plasma prolactin and two subjects reporting hot flushes compatible with an 5-HT-induced adverse effect, cortical [18F]Altanserin binding was insensitive to the citalopram challenge, even after pindolol pretreatment. The biochemical and cellular events possibly affecting the unsuccessful translation of the citalopram/pindolol challenge into a change in 5-HT2A receptor binding of [18F]Altanserin are discussed.
[¹⁸F]Altanserin and small animal PET: impact of multidrug efflux transporters on ligand brain uptake and subsequent quantification of 5-HT₂A receptor densities in the rat brain
Nucl Med Biol 2014 Jan;41(1):1-9.PMID:24120220DOI:10.1016/j.nucmedbio.2013.09.001.
Introduction: The selective 5-hydroxytryptamine type 2a receptor (5-HT(2A)R) radiotracer [(18)F]Altanserin is a promising ligand for in vivo brain imaging in rodents. However, [(18)F]Altanserin is a substrate of P-glycoprotein (P-gp) in rats. Its applicability might therefore be constrained by both a differential expression of P-gp under pathological conditions, e.g. epilepsy, and its relatively low cerebral uptake. The aim of the present study was therefore twofold: (i) to investigate whether inhibition of multidrug transporters (MDT) is suitable to enhance the cerebral uptake of [(18)F]Altanserin in vivo and (ii) to test different pharmacokinetic, particularly reference tissue-based models for exact quantification of 5-HT(2A)R densities in the rat brain. Methods: Eighteen Sprague-Dawley rats, either treated with the MDT inhibitor cyclosporine A (CsA, 50 mg/kg, n=8) or vehicle (n=10) underwent 180-min PET scans with arterial blood sampling. Kinetic analyses of tissue time-activity curves (TACs) were performed to validate invasive and non-invasive pharmacokinetic models. Results: CsA application lead to a two- to threefold increase of [(18)F]Altanserin uptake in different brain regions and showed a trend toward higher binding potentials (BP(ND)) of the radioligand. Conclusions: MDT inhibition led to an increased cerebral uptake of [(18)F]Altanserin but did not improve the reliability of BP(ND) as a non-invasive estimate of 5-HT(2A)R. This finding is most probable caused by the heterogeneous distribution of P-gp in the rat brain and its incomplete blockade in the reference region (cerebellum). Differential MDT expressions in experimental animal models or pathological conditions are therefore likely to influence the applicability of imaging protocols and have to be carefully evaluated.
Analyses of [(18)F] Altanserin bolus injection PET data. I: consideration of radiolabeled metabolites in baboons
Synapse 2001 Jul;41(1):1-10.PMID:11354008DOI:10.1002/syn.1054.
Positron emission tomography (PET) has been used to study serotonin 2A (5-HT(2A)) receptor binding in human brain using the 5-HT(2A) antagonist, [(18)F]Altanserin. Previous analyses of bolus injection [(18)F]Altanserin data provided 5-HT(2A) specific binding measures that were highly correlated with the in vitro distribution of 5-HT(2A) receptors and reflected decreased binding after ketanserin (5-HT(2A) antagonist) administration. These observations were made in the presence of a nonspecific tissue component that was consistent with blood-brain barrier (BBB) passage of radiolabeled metabolites (radiometabolites). In this work, we evaluated the in vivo kinetics of [(18)F]Altanserin and two major radiometabolites of [(18)F]Altanserin, focusing on the kinetics of free and nonspecifically-bound radioactivity. PET studies were performed in baboons after the bolus injection of [(18)F]Altanserin or one of its major radiometabolites, either [(18)F]altanserinol or [(18)F]4-(4-fluorobenzoyl)piperidine, at baseline and after pharmacologic receptor blockade (blocking data). The cerebellar and blocking data were analyzed using either single (parent radiotracer) or dual (parent radiotracer and radiometabolites) input function methods. After bolus injection of either [(18)F]Altanserin metabolite, radioactivity crossed the BBB and localized nonspecifically. The radio- metabolites were found to contribute to nonspecific "background" radioactivity that was similar in receptor-poor and receptor-rich regions. After bolus injection in baboons, two of the major radiometabolites of [(18)F]Altanserin crossed the BBB and contributed to a fairly uniform background of nonspecific radioactivity. This uniformity suggests that conventional analyses are appropriate for human bolus injection [(18)F]Altanserin PET data, although these methods may overestimate [(18)F]Altanserin nonspecific binding.
GMP-compliant radiosynthesis of [18F]Altanserin and human plasma metabolite studies
Appl Radiat Isot 2009 Apr;67(4):598-601.PMID:19162492DOI:10.1016/j.apradiso.2008.12.007.
[(18)F]Altanserin is the preferred radiotracer for in-vivo labeling of serotonin 2A receptors by positron emission tomography (PET). We report a modified synthesis procedure suited for reliable production of multi-GBq amounts of [(18)F]Altanserin useful for application in humans. We introduced thermal heating for drying of [(18)F]fluoride as well as for the reaction instead of microwave heating. We furthermore describe solid phase extraction and HPLC procedures for quantitative determination of [(18)F]Altanserin and metabolites in plasma. The time course of arterial plasma activity with and without metabolite correction was determined. 90 min after bolus injection, 38.4% of total plasma activity derived from unchanged [(18)F]Altanserin. Statistical comparison of kinetic profiles of [(18)F]Altanserin metabolism in plasma samples collected in the course of two ongoing studies employing placebo, the serotonin releaser dexfenfluramine and the hallucinogen psilocybin, revealed the same tracer metabolism. We conclude that metabolite analysis for correction of individual plasma input functions used in tracer modeling is not necessary for [(18)F]Altanserin studies involving psilocybin or dexfenfluramine treatment.