Sumatriptan succinate

Biological Activity

Sumatriptan succinate is a 5-HT1 serotonin receptor agonist. Sumatriptan reduces the vascular inflammation associated with migraine. Sumatriptan displays the highest affinity for 5-HT1D (Ki = 17 nM) and 5-HT1B (Ki = 27 nM) binding sites and is slightly less potent at 5-HT1A binding sites (Ki = 100 nM). Sumatriptan at a clinically relevant dose (100 mg/kg, s.c.) leads to a significant reduction of the mechanical allodynia-like behaviour on both the injured and the contralateral sides (peak-effects 6.3 g and 4.4 g, respectively) in a rat model of trigeminal neuropathic pain. Sumatriptan results in oral bioavailabilities of 37, 58 and 23% in rat, dog and rabbit, respectively. sumatriptan is cleared rapidly by metabolic and renal clearance with a half-life of 1-2 hour.

Product Citations

• 

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

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

• 

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

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

• 

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

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

Customer Product Validations & Biological Datas

	Source	eNeuro (2018 Jul). Figure 4. Sumatriptan (Abmole Bioscience, Houston, TX, USA)
	Method	In situ brain perfusion
	Cell Lines	Female Sprague Dawley rats
	Concentrations	0.25 μCi/ml
	Incubation Time	10 min
	Results	In contrast to the results using 14C-sucrose, uptake of 3H-sumatriptan was also robustly increased in the brainstem 1.5 h postinjection

	Source	Cephalalgia (2017). Figure 3. Sumatriptan (Abmole Bioscience, Houston, TX, USA)
	Method	s.c.
	Cell Lines	Adult male Sprague-Dawley rats
	Concentrations	3 mg/kg
	Incubation Time	2, 4 day
	Results	Saline-primed and sumatriptan-primed rats showed no significant differences in right and left CeA dynorphin levels prior to BLS exposure

	Source	Cephalalgia (2017). Figure 2. Sumatriptan (Abmole Bioscience, Houston, TX, USA)
	Method	s.c.
	Cell Lines	Adult male Sprague-Dawley rats
	Concentrations	3 mg/kg
	Incubation Time	2, 4 day
	Results	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.

	Source	Cephalalgia (2017). Figure 1. Sumatriptan (Abmole Bioscience, Houston, TX, USA)
	Method	s.c.
	Cell Lines	Adult male Sprague-Dawley rats
	Concentrations	3 mg/kg
	Incubation Time	2, 4 day
	Results	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.

	Source	Cephalalgia (2016).Figure 5. Sumatriptan succinate (Abmole Bioscience, Houston, TX, USA)
	Method	Measurement of CGRP levels
	Cell Lines
	Concentrations	0.6 mg/kg/day subcutaneously
	Incubation Time	7 days
	Results	BLS increases plasma but not CSF CGRP levels in rats with sumatriptan-induced latent sensitization.

	Source	Cephalalgia (2016).Figure 2. Sumatriptan succinate (Abmole Bioscience, Houston, TX, USA)
	Method	Evaluation of CA and Area over the time–effect curves (AOCs)
	Cell Lines
	Concentrations	0.6 mg/kg/day subcutaneously
	Incubation Time	7 days
	Results	TEV48125 blocked cutaneous allodynia evoked by bright light stress (BLS) in rats with sumatriptan-induced latent sensitization.

	Source	Cephalalgia (2016).Figure 1. Sumatriptan succinate (Abmole Bioscience, Houston, TX, USA)
	Method	Evaluation of CA and Area over the time–effect curves (AOCs)
	Cell Lines
	Concentrations	0.6 mg/kg/day subcutaneously
	Incubation Time	7 days
	Results	Dose-dependent blockade of NO donor-induced CA by TEV48125 in rats with sumatriptan-induced latent sensitization.

Protocol

Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time

Animal Experiment
Animal models	Adult male Sprague–Dawley rats model
Formulation	sterile 0.9% saline solution
Dosages	0.6 mg/kg/day for 7 days
Administration	subcutaneously injection

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Mouse	Rat	Rabbit	Guinea pig	Hamster	Dog
Weight (kg)	0.02	0.15	1.8	0.4	0.08	10
Body Surface Area (m2)	0.007	0.025	0.15	0.05	0.02	0.5
Km factor	3	6	12	8	5	20

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information

References

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.