Sumatriptan succinate 琥珀酸舒马曲坦

生物活性

Sumatriptan Succinate是一种含有磺酰胺基团的曲坦类磺胺类药物，用于治疗偏头痛。Sumatriptan对5-HT1D（Ki=17 nM）和5-HT1B结合位点（Ki= 27 nM）表现最高亲和力，对5-HT 1A结合位点（KI=100 nM）的亲和力略弱。Sumatriptan选择性收缩在偏头痛期间扩张和发炎的颅血管，这一作用由动物颅血管中的5-HT1受体亚型介导。Sumatriptan在大鼠，狗，兔中的生物活性是37％，58％和23％。Sumatriptan通过代谢和肾清除迅速清除，半衰期为1-2小时。

实验操作 来自于公开的文献，仅供相同实验参考（如实验材料、目的不同，请参考其他文献）

细胞实验
细胞系
方法
浓度
处理时间

动物实验
动物模型	Adult male Sprague–Dawley rats model
配制	sterile 0.9% saline solution
剂量	0.6 mg/kg/day for 7 days
给药处理	subcutaneously injection

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

	小鼠	大鼠	兔	豚鼠	仓鼠	狗
重量 (kg)	0.02	0.15	1.8	0.4	0.08	10
体表面积 (m2)	0.007	0.025	0.15	0.05	0.02	0.5
Km 系数	3	6	12	8	5	20

动物 A (mg/kg) = 动物 B (mg/kg) ×	动物 B的Km系数
	动物 A的Km系数

例如，依据体表面积折算法，将白藜芦醇用于小鼠的剂量22.4 mg/kg 换算成大鼠的剂量，需要将22.4 mg/kg 乘以小鼠的K_m系数（3），再除以大鼠的K_m系数（6），得到白藜芦醇用于大鼠的等效剂量为11.2 mg/kg。

化学数据

储备液配制

以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.4184 mL	12.0922 mL	24.1844 mL
5 mM	0.4837 mL	2.4184 mL	4.8369 mL
10 mM	0.2418 mL	1.2092 mL	2.4184 mL

使用AbMole产品发表的文献

• 

  Cephalalgia. 2020 Aug;40(9):892-902.

  Ubrogepant does not induce latent sensitization in a preclinical model of medication overuse headache
  Sumatriptan succinate购买自AbMole

• 

  Cephalalgia. 2020 Aug;40(9):903-912.

  Evaluation of LY573144 (lasmiditan) in a preclinical model of medication overuse headache
  Sumatriptan succinate购买自AbMole

• 

  eNeuro. 2018 July 5;0116-18.

  Loss of Blood-Brain Barrier Integrity in a KCl-Induced Model of Episodic Headache Enhances CNS Drug Delivery
  Sumatriptan succinate购买自AbMole

• 

  Cephalalgia. 2017 Jul;37(8):780-794.

  Kappa opioid receptor antagonists: A possible new class of therapeutics for migraine prevention
  Sumatriptan succinate购买自AbMole

• 

  Cephalalgia. 2016 May 19.

  Prevention of stress- or nitric oxide donor-induced medication overuse headache by a calcitonin gene-related peptide antibody in rodents.
  Sumatriptan succinate购买自AbMole

客户产品验证及相关生物数据

	数据来源	eNeuro (2018 Jul). Figure 4. Sumatriptan (Abmole Bioscience, Houston, TX, USA)
	方法	In situ brain perfusion
	细胞系	Female Sprague Dawley rats
	浓度	0.25 μCi/ml
	处理时间	10 min
	实验结果	In contrast to the results using 14C-sucrose, uptake of 3H-sumatriptan was also robustly increased in the brainstem 1.5 h postinjection

	数据来源	Cephalalgia (2017). Figure 3. Sumatriptan (Abmole Bioscience, Houston, TX, USA)
	方法	s.c.
	细胞系	Adult male Sprague-Dawley rats
	浓度	3 mg/kg
	处理时间	2, 4 day
	实验结果	Saline-primed and sumatriptan-primed rats showed no significant differences in right and left CeA dynorphin levels prior to BLS exposure

	数据来源	Cephalalgia (2017). Figure 2. Sumatriptan (Abmole Bioscience, Houston, TX, USA)
	方法	s.c.
	细胞系	Adult male Sprague-Dawley rats
	浓度	3 mg/kg
	处理时间	2, 4 day
	实验结果	The AOC data from periorbital and hindpaw threshold (Figure 2 (c) and (d)) also demonstrated that CYM51317 (20mg/kg, p.o.) administration abolished stress-induced cutaneous allodynia in sumatriptan-primed rats.

	数据来源	Cephalalgia (2017). Figure 1. Sumatriptan (Abmole Bioscience, Houston, TX, USA)
	方法	s.c.
	细胞系	Adult male Sprague-Dawley rats
	浓度	3 mg/kg
	处理时间	2, 4 day
	实验结果	Sumatriptan exposure with s.c. vehicle injections followed by BLS resulted in a significant reduction in periorbital thresholds, indicative of cutaneous allodynia, at 2 and 3 h after BLS.

	数据来源	Cephalalgia (2016).Figure 5. Sumatriptan succinate (Abmole Bioscience, Houston, TX, USA)
	方法	Measurement of CGRP levels
	细胞系
	浓度	0.6 mg/kg/day subcutaneously
	处理时间	7 days
	实验结果	BLS increases plasma but not CSF CGRP levels in rats with sumatriptan-induced latent sensitization.

	数据来源	Cephalalgia (2016).Figure 2. Sumatriptan succinate (Abmole Bioscience, Houston, TX, USA)
	方法	Evaluation of CA and Area over the time–effect curves (AOCs)
	细胞系
	浓度	0.6 mg/kg/day subcutaneously
	处理时间	7 days
	实验结果	TEV48125 blocked cutaneous allodynia evoked by bright light stress (BLS) in rats with sumatriptan-induced latent sensitization.

	数据来源	Cephalalgia (2016).Figure 1. Sumatriptan succinate (Abmole Bioscience, Houston, TX, USA)
	方法	Evaluation of CA and Area over the time–effect curves (AOCs)
	细胞系
	浓度	0.6 mg/kg/day subcutaneously
	处理时间	7 days
	实验结果	Dose-dependent blockade of NO donor-induced CA by TEV48125 in rats with sumatriptan-induced latent sensitization.

参考文献

Prevention of stress- or nitric oxide donor-induced medication overuse headache by a calcitonin gene-related peptide antibody in rodents.
Kopruszinski CM, et al. Cephalalgia. 2016 May 19. PMID: 27206958.