Spiramide AMI-193|cas:510-74-7|西域试剂

Spiramide AMI-193,98.81%

产品编号：Bellancom-100971| CAS NO：510-74-7| 分子式：C₂₂H₂₆FN₃O₂| 分子量：383.46

Spiramide (AMI-193) 是一种有效和选择性的 5-HT2 和 dopamine D2 受体拮抗剂，Ki 值分别为 2 nM 和 3 nM。Spiramide 对 5-HT2 受体的选择性与 5-HT1C 受体 (Ki=4300 nM) 相比大于 2000 倍。Spiramide 具有抗精神病活性。

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货号	价格	库存与货期
Bellancom-100971	￥800.00	杭州北京（现货）
Bellancom-100971	￥1300.00	杭州北京（现货）
Bellancom-100971	￥2800.00	杭州北京（现货）
Bellancom-100971	￥4500.00	杭州北京（现货）
Bellancom-100971	￥7500.00	杭州北京（现货）

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Spiramide AMI-193

产品介绍

Spiramide (AMI-193) 是一种有效和选择性的 5-HT₂ 和 dopamine D2 受体拮抗剂，K_i 值分别为 2 nM 和 3 nM。Spiramide 对 5-HT2 受体的选择性与 5-HT_1C 受体 (K_i=4300 nM) 相比大于 2000 倍。Spiramide 具有抗精神病活性。

生物活性

Spiramide (AMI-193) is a potent and selective antagonist of 5-HT₂ and dopamine D2 receptor, with K_is of 2 nM and 3 nM, respectively. Spiramide has >2000-fold selectivity for 5-HT₂ versus 5-HT_1C (K_i=4300 nM) receptors. Spiramide exhibits antipsychotic activity.

体外研究

Spiramide retains affinity for 5-HT_1A sites (K_i=50 nM) and also binds at dopamine D2 sites (K_i=3 nM), but possesses low affinity for dopamine D1 sites (K_i=2530 nM).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

AMI-193 (0.003-0.01 mg/kg; i.m.) dose-dependently decreases response rate in monkeys under a fixed-interval (FI) schedule of stimulus termination.
AMI-193 (0.003-0.01 mg/kg; i.m.) attenuates the discriminative-stimulus effects of cocaine in drug-discrimination experiments.
AMI-193 (0.003-0.01 mg/kg; i.m.) reduces response rate under a second-order schedule of i.v. self-administration of cocaine (0.1 mg/infusion).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Adult male squirrel monkeys (850-1300 g)
Dosage:	0.003, 0.01 mg/kg
Administration:	I.m. on Tuesday, Wednesday, and Thursday the following week
Result:	Decreased the response rate. The rate-decreasing effects were reversed by cocaine.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Adult male squirrel monkeys (850-1300 g)
Dosage:	0.003, 0.01 mg/kg
Administration:	I.m. on Tuesday, Wednesday, and Thursday the following week
Result:	Decreased the response rate. The rate-decreasing effects were reversed by cocaine.

性状

Solid

溶解性数据

In Vitro:

DMSO : 20 mg/mL (52.16 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6078 mL	13.0392 mL	26.0783 mL
5 mM	0.5216 mL	2.6078 mL	5.2157 mL
10 mM	0.2608 mL	1.3039 mL	2.6078 mL

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, 6 months; -20°C, 1 month (stored under nitrogen)。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2 mg/mL (5.22 mM); Clear solution

此方案可获得 ≥ 2 mg/mL (5.22 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2 mg/mL (5.22 mM); Suspended solution; Need ultrasonic

此方案可获得 2 mg/mL (5.22 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

*以上所有助溶剂都可在西域网站选购。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

参考文献

. Ismaiel AM, et, al. Antagonism of 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane stimulus with a newly identified 5-HT2- versus 5-HT1C-selective antagonist. J Med Chem. 1993 Aug 20;36(17):2519-25. [Content Brief]

. Czoty PW, et, al. Behavioral effects of AMI-193, a 5-HT(2A)- and dopamine D(2)-receptor antagonist, in the squirrel monkey. Pharmacol Biochem Behav. 2000 Oct;67(2):257-64. [Content Brief]

. Kjellberg B, et, al. Partial restoration by a neuroleptic (spiramide) of items of grooming behaviour suppressed by amphetamine. Arch Int Pharmacodyn Ther. 1974 Jul;210(1):61-6. [Content Brief]

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Spiramide AMI-193,98.81%

Spiramide AMI-193

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