U-54,494A
| U-54494A_structure.png | |
U-54,494A is a synthetic opioid analgesic that was developed in the 1970s by the Upjohn Company. It is part of a class of compounds known as benzomorphans, which are structurally distinct from other opioid classes such as morphinans and phenylpiperidines. U-54,494A is notable for its potent analgesic effects and its unique pharmacological profile.
Pharmacology[edit | edit source]
U-54,494A acts primarily as a kappa-opioid receptor agonist, which is responsible for its analgesic properties. Unlike many other opioids, which primarily target the mu-opioid receptor, kappa-opioid receptor agonists like U-54,494A can produce analgesia without the same degree of respiratory depression or addiction potential. However, kappa agonists are also associated with dysphoria and hallucinations, which can limit their clinical use.
Mechanism of Action[edit | edit source]
The analgesic effects of U-54,494A are mediated through its action on the kappa-opioid receptors in the central nervous system. Activation of these receptors leads to inhibition of neurotransmitter release and modulation of pain pathways. This mechanism is distinct from that of mu-opioid receptor agonists, which primarily inhibit pain by acting on different neural circuits.
Side Effects[edit | edit source]
Common side effects of kappa-opioid receptor agonists, including U-54,494A, include dysphoria, hallucinations, and sedation. These effects are thought to result from the activation of kappa receptors in brain regions associated with mood and perception.
Research and Development[edit | edit source]
U-54,494A was initially investigated for its potential as a non-addictive analgesic. However, the development of this compound was limited by its side effect profile. Research into kappa-opioid receptor agonists continues, with the aim of developing compounds that retain analgesic efficacy while minimizing adverse effects.
Legal Status[edit | edit source]
U-54,494A is not currently approved for medical use and is primarily of interest in research settings. Its legal status may vary by country, and it is important for researchers to be aware of local regulations regarding its use.
Also see[edit | edit source]
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
