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Sumatriptan succinate

Cat. No. M2048
Sumatriptan succinate Structure
Synonym:

GR-43175

Size Price Availability Quantity
100mg USD 105 In stock
500mg USD 280 In stock
1g USD 460 In stock
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Quality Control
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.

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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 413.49
Formula C14H21N3O2S.C4H6O4
CAS Number 103628-48-4
Purity 100.00%
Solubility DMSO 80 mg/mL
Water 80 mg/mL
Storage at -20°C
Customer Product Validations & Biological Datas
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.
Rating
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.
Rating
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.
Rating
Product Citations
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.

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  Catalog
Abmole Inhibitor Catalog 2017




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