Evaluation of a series of N-alkyl benzomorphans in cell lines expressing transfected delta- and mu-opioid receptors

Biochemical Pharmacology
M E AboodL S Harris


Transfection of individual opioid receptors in Chinese hamster ovary (CHO) cells provides a pure, homogeneous population of receptors for screening drug candidates, and an alternative to the use of selective ligands. To evaluate the potential of this system, we chose a series of (-)-5,9 alpha-dimethyl-2-hydroxy-N-substituted-6,7-benzomorphans, for which the receptor selectivity and in vivo activity had been characterized recently, and tested them in CHO cells stably transfected with either the rat delta-opioid receptor or the mouse mu-opioid receptor. [3H]Diprenorphine was used to measure opioid receptors in P2 membrane preparations. A Bmax of 7.58 +/- 0.8 pmol/mg protein and a Kd of 0.42 +/- 0.04 nM was obtained in the mu-opioid receptor expressing cell line used in these studies. In addition, [3H]naltrindole was used to confirm the delta-specificity of the cloned receptor. Both compounds gave a Bmax of 1.2 pmol/mg in the CHO cells expressing the rat delta-opioid receptor. Displacement assays were performed with eleven (-)-N-alkyl-benzomorphans in the absence and presence of 150 mM NaCl, as well as known delta- and mu-selective agonists. Sodium reduced agonist affinity in the transfected cell lines. The benzomorphan compounds ...Continue Reading


Apr 1, 1978·Proceedings of the National Academy of Sciences of the United States of America·A J Blume
Dec 15, 1992·Proceedings of the National Academy of Sciences of the United States of America·B L KiefferC G Hirth
Dec 28, 1992·Science·C J EvansR H Edwards
Mar 1, 1994·Trends in Neurosciences·G R UhlG Pasternak
Apr 15, 1994·Journal of Neuroscience Research·M E AboodQ Tao
Aug 15, 1994·Biochemical and Biophysical Research Communications·E ManssonD Yang
Apr 26, 1994·Proceedings of the National Academy of Sciences of the United States of America·G X XieH Akil
Jun 1, 1994·Journal of Neurochemistry·R L ZastawnyB F O'Dowd
Nov 1, 1993·Proceedings of the National Academy of Sciences of the United States of America·J B WangG R Uhl
Nov 1, 1993·Proceedings of the National Academy of Sciences of the United States of America·F MengH Akil
Nov 1, 1993·The Biochemical Journal·S LiL Y Liu-Chen
Jul 15, 1993·Proceedings of the National Academy of Sciences of the United States of America·K YasudaG I Bell

❮ Previous
Next ❯

Related Concepts

Trending Feeds


Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.


Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.


Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.

Related Papers

The Journal of Pharmacy and Pharmacology
M D Aceto, P C Zenk
Antonio Lazcano, Kevin P Hand
© 2021 Meta ULC. All rights reserved