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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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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. |
| 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 |
| 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 |
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Tegaserod is an orally active serotonin receptor 4 (5-HT4R) agonist and a 5-HT2B receptor antagonist. Tegaserod has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively. Tegaserod causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. |
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