abstract |
Substituted pyrazoles, imidazoles, triazoles, other 5-membered heteroaromatic ring compounds, substituted 6-membered heteroaromatic ring compounds, fluorene and carbazole compounds, and pyrazoles, imidazoles, triazoles, and other 5- membered heteroaromatic ring compounds substituted with two phenyl groups, may be used as selective peripheral opioid-receptor agonists and antagonist that are designed to elicit the pharmacological effects through the peripheral opioid receptors. These compounds compete with opioid analgesics for binding sites on opioid receptors and particularly the delta and mu opioid receptors, but are unable to cross the blood-brain barrier. Such compounds and pharmaceutical compositions comprising such compounds offer methods of treatment of conditions mediated by opioid receptors, including postoperative and chronic pain, and cytoprotection. |