Elzasonan Explained

Elzasonan (CP-448,187) is a selective 5-HT_1B and 5-HT_1D receptor antagonist that was under development by Pfizer for the treatment of depression but was discontinued, possibly due to poor efficacy.^{[1] [2] [3] [4] [5]} By preferentially blocking 5-HT_1B and 5-HT_1D autoreceptors, elzasonan is thought to enhance serotonergic innervations originating from the raphe nucleus, thereby improving signaling to limbic regions like the hippocampus and prefrontal cortex and ultimately resulting in antidepressant effects.^[3]

See also

• GR-127,935
• SB-649,915

Notes and References

1. Book: Vela JM, Buschmann H, Holenz J, Párraga A, Torrens A . Antidepressants, Antipsychotics, Anxiolytics: From Chemistry and Pharmacology to Clinical Application . Wiley-VCH . Weinheim . 2007 . 978-3-527-31058-6 .
2. Book: Stahl SM . Stahl's essential psychopharmacology: neuroscientific basis and practical applications . Cambridge University Press . Cambridge, UK . 2008 . 978-0-521-85702-4 .
3. Dawson LA, Bromidge SM . 5-HT1 receptor augmentation strategies as enhanced efficacy: therapeutics for psychiatric disorders . Current Topics in Medicinal Chemistry . 8 . 12 . 1008–1023 . August 2008 . 18691129 . 10.2174/156802608785161439 .
4. Pfizer, Inc.: analysis of patenting 1998 – 2001 . Expert Opinion on Therapeutic Patents. 12. 5. 725–732. 10.1517/13543776.12.5.725 . 2002. Norman P . 84645020. vanc .
5. Kirchhoff VD, Nguyen HT, Soczynska JK, Woldeyohannes H, McIntyre RS . Discontinued psychiatric drugs in 2008 . Expert Opinion on Investigational Drugs . 18 . 10 . 1431–1443 . October 2009 . 19715445 . 10.1517/13543780903184591 . 34201544 .