Delta opioid binding selectivity of 3-ether analogs of naltrindole

A Coop; J Pinto; L Wang; K McCullough; R B Rothman; C Dersch; A E Jacobson; K C Rice

doi:10.1016/s0960-894x(99)00622-8

Delta opioid binding selectivity of 3-ether analogs of naltrindole

Bioorg Med Chem Lett. 1999 Dec 20;9(24):3435-8. doi: 10.1016/s0960-894x(99)00622-8.

Authors

A Coop¹, J Pinto, L Wang, K McCullough, R B Rothman, C Dersch, A E Jacobson, K C Rice

Affiliation

¹ Laboratory of Medicinal Chemistry, National Institute of Diabetes, Digestive and Kidney Diseases, Bethesda, MD 20892, USA.

PMID: 10617086
DOI: 10.1016/s0960-894x(99)00622-8

Abstract

Masking of the 3-phenol of naltrindole as a range of ethers caused a decrease in binding affinity at all three opiate receptors (mu, kappa, delta), however for the methyl ether, the reduction in affinity at both mu and kappa was greater than at delta, thereby increasing delta binding selectivity.

MeSH terms

Naltrexone / analogs & derivatives*
Naltrexone / chemistry
Naltrexone / metabolism
Narcotic Antagonists / chemistry
Narcotic Antagonists / metabolism*
Protein Binding
Receptors, Opioid, delta / metabolism*

Substances

Narcotic Antagonists
Receptors, Opioid, delta
Naltrexone
naltrindole