Chemistry:Terbogrel

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Terbogrel
Terbogrel.svg
Names
IUPAC name
(5E)-6-{3-[tert-Butyl(cyano)carbamimidamido]phenyl}-6-pyridin-3-ylhex-5-enoic acid
Other names
(5E)-6-[m-(3-tert-Butyl-2-cyanoguanidino)phenyl]-6-(3-pyridyl)-5-hexenoic acid
Identifiers
3D model (JSmol)
ChEMBL
ChemSpider
KEGG
UNII
Properties
C23H27N5O2
Molar mass 405.502 g·mol−1
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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Infobox references

Terbogrel (INN[1]) is an experimental drug that has been studied for its potential to prevent the vasoconstricting and platelet-aggregating action of thromboxanes. Terbogrel is an orally available thromboxane A2 receptor antagonist and a thromboxane A synthase inhibitor.[2][3] The drug was developed by Boehringer Ingelheim.

A phase 2 clinical trial of terbogrel was discontinued due to its induction of leg pain.[4]

See also

References

  1. "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names (Rec. INN): List 37". WHO Drug Information 11 (1): 49. 1997. http://apps.who.int/medicinedocs/index/assoc/s14162e/s14162e.pdf. Retrieved 3 December 2016. 
  2. Guth, BD; Narjes, H; Schubert, HD; Tanswell, P; Riedel, A; Nehmiz, G (July 2004). "Pharmacokinetics and Pharmacodynamics of Terbogrel, a Combined Thromboxane A2 Receptor and Synthase Inhibitor, in Healthy Subjects". British Journal of Clinical Pharmacology 58 (1): 40–51. doi:10.1111/j.1365-2125.2004.02083.x. PMID 15206991. 
  3. Michaux, C; Norberg, B; Dogné, JM; Durant, F; Masereel, B; Delarge, J; Wouters, J (October 2000). "Terbogrel, a Dual-Acting Agent for Thromboxane Receptor Antagonism and Thromboxane Synthase Inhibition". Acta Crystallographica 56 (Pt 10): 1265–6. doi:10.1107/s0108270100009872. PMID 11025320. 
  4. "Impact of vascular thromboxane prostanoid receptor activation on hemostasis, thrombosis, oxidative stress, and inflammation". Journal of Thrombosis and Haemostasis 12 (2): 126–37. 2014. doi:10.1111/jth.12472. PMID 24298905.