Free shipping on all orders over $ 500

Sumatriptan succinate

Cat. No. M2048
Sumatriptan succinate Structure
Synonym:

GR-43175

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
50mg USD 76  USD76 In stock
100mg USD 96  USD96 In stock
500mg USD 286  USD286 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
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
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 (for reference only)
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
Chemical Information
Molecular Weight 413.49
Formula C14H21N3O2S.C4H6O4
CAS Number 103628-48-4
Solubility (25°C) DMSO 50 mg/mL
Water 40 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Kopruszinski CM, et al. Cephalalgia. Prevention of stress- or nitric oxide donor-induced medication overuse headache by a calcitonin gene-related peptide antibody in rodents.

Related 5-HT Receptor Products
Thiothixene

Thiothixene is a thianthrene derivative, a dopamine antagonist with antipsychotic properties. It has been used in studies of psychiatric disorders, such as schizophrenia.

SEP-363856

SEP-363856 (SEP-856) is an orally active, CNS-active antipsychotic active compound with potential for the study of schizophrenia.

Perospirone

Perospirone (SM-9018 free base) is an orally active antagonist of 5-hydroxytryptamine2 (5-HT2) receptor, dopamine2 (D2) receptor and 5-HT1A receptor with Ki of 0.6 nM, 1.4 nM and 2.9 nM, respectively.

SB 200646

SB 200646 (SB 200646A) is a potent, selective and oral-active antagonist of 5-HT2B/2C over 5-HT2A receptor with 50 fold selectivity. The pKi for rat 5-HT2C receptor, rat 5-HT2B receptor and rat 5-HT2A receptor are 6.9, 7.5 and 5.2, respectively. SB 200646 has electrophysiological and anxiolytic properties in vivo.

Lvguidingan

Lvguidingan (Anticonvulsant 7903) is an anticonvulsant/antiepileptic agent. Lvguidingan (Anticonvulsant 7903) is found to be able to increase the concentration of 5-HT and 5-HIAA in mice brain.

  Catalog
Abmole Inhibitor Catalog




Keywords: Sumatriptan succinate, GR-43175 supplier, 5-HT Receptor, inhibitors, activators

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.