Thioperamide
Thioperamide is a histamine H3 receptor antagonist with Ki values of 4.3 nM at the H3 receptor and 31 nM at the H4 receptor. It has been used in scientific research to help elucidate the function of the histamine H3 receptor, with the development of a radiolabelled form of thioperamide allowing the distribution of H3 receptors in the brain to be mapped by autoradiography.
Chemistry[edit | edit source]
Thioperamide is a derivative of imidazole, a common scaffold in pharmacology due to its ability to mimic the structure of histamine. The methyl group attached to the imidazole ring of thioperamide is thought to interact with a lipophilic binding pocket on the H3 receptor, enhancing its affinity for the receptor.
Pharmacology[edit | edit source]
Thioperamide acts as an antagonist at the histamine H3 receptor, meaning it binds to the receptor and prevents it from being activated by histamine. This has the effect of increasing the release of histamine in the brain, as the H3 receptor normally acts to inhibit histamine release. Thioperamide also has some affinity for the H4 receptor, although it is less potent at this receptor than at the H3 receptor.
Clinical significance[edit | edit source]
The ability of thioperamide to increase histamine release in the brain has led to it being investigated for potential use in the treatment of neurological disorders such as Alzheimer's disease and narcolepsy. However, due to its poor bioavailability and the presence of side effects such as insomnia and anxiety, thioperamide has not been developed for clinical use.
See also[edit | edit source]
| Thioperamide Resources | |
|---|---|
|
 |
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
