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.
Cephalalgia. 2021 Sep 12;3331024211039813.
A prolactin-dependent sexually dimorphic mechanism of migraine chronification
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
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
eNeuro. 2018 July 5;5(4):ENEURO.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
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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 |
Molecular Weight | 413.49 |
Formula | C14H21N3O2S.C4H6O4 |
CAS Number | 103628-48-4 |
Solubility (25°C) | DMSO 50 mg/mL Water 90 mg/mL |
Storage | -20°C, dry, sealed |
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 Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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MM120
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