General description
An antagonist of the 5-HT2B (pki = 8.0-9.4) and 5-HT2C (pki = 8.6-9.1) receptor. At the 5-HT1A and some other 5-HT receptors it serves as a partial agonist. It is known to have partial agonist effects on other 5-HT receptors as well. In neuronal and platelet culture, Methysergide blocks serotonin action with an IC50 = 18 µM. Originally developed in the 1960′s as a migraine/cluster headache treatment, but discontinued due to significant physiological and pyschotropic side effects. Methysergide is still actively used in research as a 5-HT2 receptor antagonist in both in vivo and in vitro experiments.
Biochem/physiol Actions
Primary Target
5-HT
Warning
Toxicity: Toxic (F)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Due to the nature of the Hazardous Materials in this shipment, additional shipping charges may be applied to your order. Certain sizes may be exempt from the additional hazardous materials shipping charges. Please contact your local sales office for more information regarding these charges.
Matsuta, Y. et al. 2013. Exp. Neurol.247, 250.
IUHPAR Database 2013.
Shad, K.F., Saeed, S.A. 2007. Exp. Brain Res.183, 411.
Knight, A.R. et al. 2004. Naunyn Schmiedebergs Arch. Pharmacol.370, 114.
Saxena, P.R and Lawang, A. 1985. Arch. Int. Pharmacodyn. Ther.277, 235.
Colpaert, F. C. et al. 1979. Eur. J. Pharmacol.58, 505.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Shipping Information:
Hazmat Fee: $65.00 + applicable shipping charges are added after the order is placed.
More Information: https://cenmed.com/shipping-returns
- UPC:
- 51142431
- Condition:
- New
- Availability:
- 3-5 Days
- Weight:
- 1.00 Ounces
- HazmatClass:
- Yes
- MPN:
- 5064190001
- CAS:
- 129-49-7