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Trelanserin

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Trelanserin
Clinical data
Other namesSL 65.0472; SL-650472; SL650472
Routes of
administration		Oral[1]
Drug classSerotonin 5-HT1B receptor antagonist; Serotonin 5-HT2A receptor antagonist; Anticoagulant
ATC code
  • None
Identifiers
  • 2-[7-fluoro-2-oxo-4-[2-(4-thieno[3,2-c]pyridin-4-ylpiperazin-1-yl)ethyl]quinolin-1-yl]acetamide
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC24H24FN5O2S
Molar mass465.55 g·mol−1
3D model (JSmol)
  • C1CN(CCN1CCC2=CC(=O)N(C3=C2C=CC(=C3)F)CC(=O)N)C4=NC=CC5=C4C=CS5
  • InChI=1S/C24H24FN5O2S/c25-17-1-2-18-16(13-23(32)30(15-22(26)31)20(18)14-17)4-7-28-8-10-29(11-9-28)24-19-5-12-33-21(19)3-6-27-24/h1-3,5-6,12-14H,4,7-11,15H2,(H2,26,31)
  • Key:JDLYOFUDIKMYBL-UHFFFAOYSA-N

Trelanserin (INNTooltip International Nonproprietary Name; developmental code name SL 65.0472) is a dual serotonin 5-HT1B receptor antagonist and serotonin 5-HT2A receptor antagonist which was under development for the treatment of peripheral arterial occlusive disorders and thrombosis but was never marketed.[1][2][3][4] It is taken orally.[1] The drug was under development by Sanofi-Aventis.[1][2] It reached phase 2 clinical trials prior to the discontinuation of its development in 2009.[1][2][3] Trelanserin was first described in the scientific literature by 2000.[5]

See also

[edit]

References

[edit]
  1. ^ a b c d e "SL 650472". AdisInsight. 13 March 2009. Retrieved 16 January 2026.
  2. ^ a b c "Delving into the Latest Updates on Trelanserin with Synapse". Synapse. 25 October 2025. Retrieved 16 January 2026.
  3. ^ a b Zhang XS, Xiang BR (July 2009). "Discontinued drugs in 2008: cardiovascular drugs". Expert Opinion on Investigational Drugs. 18 (7): 875–885. doi:10.1517/13543780903020308. PMID 19548849. 2.3.10 SL-65.0472 (SL-650472, SL650472) SL-65.0472 (SL-650472, SL650472; Sanofi-Aventis) is a 5HT1B/2A antagonist for the treatment of PAO. The molecule prevents local vasoconstriction and platelet aggregation and has antiproliferative activity at sites where atherosclerotic endothelium is present. The compound was in Phase IIb trial (MASCOT) in intermittent claudication Fontaine Stage II patients. However, it has been discontinued due to an inadequate risk–reward profile.
  4. ^ Berry CN, Lorrain J, Lochot S, Delahaye M, Lalé A, Savi P, et al. (March 2001). "Antiplatelet and antithrombotic activity of SL65.0472, a mixed 5-HT1B/5-HT2A receptor antagonist". Thrombosis and Haemostasis. 85 (3). Thromb Haemost: 521–528. doi:10.1055/s-0037-1615615. PMID 11307825.
  5. ^ Galzin AM, Delahaye M, Hoornaert C, McCort G, O'Connor SE (September 2000). "Effects of SL 65.0472, a novel 5-HT receptor antagonist, on 5-HT receptor mediated vascular contraction". European Journal of Pharmacology. 404 (3). Elsevier BV: 361–368. doi:10.1016/s0014-2999(00)00630-0. PMID 10996601.
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