5'-Guanidinonaltrindole TFA is a selective antagonist of the kappa-opioid receptor, demonstrating significant opioid antagonist activity. It exhibits an antagonistic potency five times greater than that of norbinatorphimine in smooth muscle preparations, with a selectivity ratio exceeding 500-fold. Binding and functional studies reveal pA(2) values aligning with the smooth muscle data, indicating its effectiveness. This compound serves as a valuable pharmacological tool for investigating the role of kappa-opioid receptors in opioid research.
5'-Guanidinonaltrindole TFA is a selective antagonist of the kappa-opioid receptor, demonstrating significant opioid antagonist activity. It exhibits an antagonistic potency five times greater than that of norbinatorphimine in smooth muscle preparations, with a selectivity ratio exceeding 500-fold. Binding and functional studies reveal pA(2) values aligning with the smooth muscle data, indicating its effectiveness. This compound serves as a valuable pharmacological tool for investigating the role of kappa-opioid receptors in opioid research.
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