Siramesine
Siramesine (or Lu 28-179) is a sigma receptor agonist, selective for the σ2 subtype.[1] In animal studies, siramesine has been shown to produce anxiolytic[2] and antidepressant[3] effects. It was developed by the pharmaceutical company H Lundbeck for the treatment of anxiety,[4] although development was discontinued after clinical trials showed a lack of efficacy in humans.
Siramesine has been shown to produced an enhanced antidepressant effect when co-administered with NMDA antagonists.[5] It has also been used to study the σ2 activity of cocaine,[6] and has been shown to produce anticancer properties both in vitro[7] and in vivo.[8]
References[edit | edit source]
- ↑ Soby KK, Mikkelsen JD, Meier E, Thomsen C. Lu 28-179 labels a sigma(2)-site in rat and human brain. Neuropharmacology. 2002 Jul;43(1):95-100.
- ↑ Sanchez C, Arnt J, Costall B, Kelly ME, Meier E, Naylor RJ, Perregaard J. The selective sigma2-ligand Lu 28-179 has potent anxiolytic-like effects in rodents. Journal of Pharmacology and Experimental Therapeutics. 1997 Dec;283(3):1323-32.
- ↑ Sanchez C, Papp M. The selective sigma2 ligand Lu 28-179 has an antidepressant-like profile in the rat chronic mild stress model of depression. Behavioural Pharmacology. 2000 Apr;11(2):117-24.
- ↑ Heading C. Siramesine H Lundbeck. Current Opinion in Investigational Drugs. 2001 Feb;2(2):266-70.
- ↑ Skuza G, Rogoz Z. The synergistic effect of selective sigma receptor agonists and uncompetitive NMDA receptor antagonists in the forced swim test in rats. Journal of Physiology and Pharmacology. 2006 Jun;57(2):217-29.
- ↑ Nuwayhid SJ, Werling LL. Sigma2 (σ2) receptors as a target for cocaine action in the rat striatum. European Journal of Pharmacology. 2006 Mar 27;535(1-3):98-103.
- ↑ Ostenfeld MS, Fehrenbacher N, Hoyer-Hansen M, Thomsen C, Farkas T, Jaattela M. Effective tumor cell death by sigma-2 receptor ligand siramesine involves lysosomal leakage and oxidative stress. Cancer Research. 2005 Oct 1;65(19):8975-83.
- ↑ Groth-Pedersen L, Ostenfeld MS, Hoyer-Hansen M, Nylandsted J, Jaattela M. Vincristine induces dramatic lysosomal changes and sensitizes cancer cells to lysosome-destabilizing siramesine. Cancer Research. 2007 Mar 1;67(5):2217-25.
External links[edit | edit source]
- Siramesine at the US National Library of Medicine Medical Subject Headings (MeSH)
 | This pharmacology-related article is a stub. You can help WikiMD by expanding it. |
Search WikiMD
Ad.Tired of being Overweight? Try W8MD's physician weight loss program.
Semaglutide (Ozempic / Wegovy and Tirzepatide (Mounjaro / Zepbound) available.
Advertise on WikiMD
|
WikiMD's Wellness Encyclopedia |
| Let Food Be Thy Medicine Medicine Thy Food - Hippocrates |
Translate this page: - East Asian
中文,
日本,
한국어,
South Asian
हिन्दी,
தமிழ்,
తెలుగు,
Urdu,
ಕನ್ನಡ,
Southeast Asian
Indonesian,
Vietnamese,
Thai,
မြန်မာဘာသာ,
বাংলা
European
español,
Deutsch,
français,
Greek,
português do Brasil,
polski,
română,
русский,
Nederlands,
norsk,
svenska,
suomi,
Italian
Middle Eastern & African
عربى,
Turkish,
Persian,
Hebrew,
Afrikaans,
isiZulu,
Kiswahili,
Other
Bulgarian,
Hungarian,
Czech,
Swedish,
മലയാളം,
मराठी,
ਪੰਜਾਬੀ,
ગુજરાતી,
Portuguese,
Ukrainian
Medical Disclaimer: WikiMD is not a substitute for professional medical advice. The information on WikiMD is provided as an information resource only, may be incorrect, outdated or misleading, and is not to be used or relied on for any diagnostic or treatment purposes. Please consult your health care provider before making any healthcare decisions or for guidance about a specific medical condition. WikiMD expressly disclaims responsibility, and shall have no liability, for any damages, loss, injury, or liability whatsoever suffered as a result of your reliance on the information contained in this site. By visiting this site you agree to the foregoing terms and conditions, which may from time to time be changed or supplemented by WikiMD. If you do not agree to the foregoing terms and conditions, you should not enter or use this site. See full disclaimer.
Credits:Most images are courtesy of Wikimedia commons, and templates Wikipedia, licensed under CC BY SA or similar.
Contributors: Prab R. Tumpati, MD
