GR-103545
| GR-103545_structure.png | |
GR-103545 is a chemical compound that acts as a potent and selective kappa-opioid receptor (KOR) agonist. It has been primarily studied for its potential use in treating conditions such as pain, depression, and addiction.
Pharmacology[edit | edit source]
GR-103545 is known for its high affinity and selectivity for the kappa-opioid receptor, a type of opioid receptor that is involved in modulating pain perception, mood, and stress responses. Unlike mu-opioid receptor agonists, which are commonly associated with addictive properties and respiratory depression, kappa-opioid receptor agonists like GR-103545 are being investigated for their potential to provide analgesia without these side effects.
Mechanism of Action[edit | edit source]
The kappa-opioid receptor is a G-protein coupled receptor (GPCR) that, when activated by agonists such as GR-103545, inhibits adenylate cyclase activity, reduces cAMP levels, and modulates ion channel activity. This leads to decreased neuronal excitability and neurotransmitter release, contributing to its analgesic and mood-altering effects.
Therapeutic Potential[edit | edit source]
Research into GR-103545 has suggested its potential utility in several therapeutic areas:
- Pain Management: As a kappa-opioid receptor agonist, GR-103545 may provide effective pain relief without the risk of addiction associated with traditional opioids.
- Depression: Kappa-opioid receptor agonists have been studied for their antidepressant effects, potentially offering a novel mechanism for treating mood disorders.
- Addiction: There is interest in using kappa-opioid receptor agonists to reduce cravings and withdrawal symptoms in individuals with substance use disorders.
Research and Development[edit | edit source]
While GR-103545 has shown promise in preclinical studies, its development has been limited by side effects such as dysphoria and hallucinations, which are common with kappa-opioid receptor agonists. Ongoing research aims to develop compounds that retain the therapeutic benefits while minimizing adverse effects.
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
