Affinity of fentanyl and its derivatives for the σ1-receptor.
@article{Lipiski2019AffinityOF, title={Affinity of fentanyl and its derivatives for the σ1-receptor.}, author={Piotr F. J. Lipiński and E. Szűcs and Małgorzata Jarończyk and P. Kosson and S. Benyhe and A. Misicka and J. Dobrowolski and Joanna Sadlej}, journal={MedChemComm}, year={2019}, volume={10 7}, pages={ 1187-1191 } }
Fentanyl and its 11 commercially available derivatives were investigated as to their affinity for the σ1 receptor. The parent compound is a rather poor binder (IC50 = 4973 nM), but its close derivatives (benzylfentanyl or p-fluorofentanyl) have submicromolar affinities. Modelling provides a structural basis for the observed trends in activity.
Topics from this paper
References
SHOWING 1-10 OF 25 REFERENCES
Fentanyl Family at the Mu-Opioid Receptor: Uniform Assessment of Binding and Computational Analysis
- Chemistry, Medicine
- Molecules
- 2019
- 10
- PDF
Pharmacology and Therapeutic Potential of Sigma1 Receptor Ligands
- Medicine
- Current neuropharmacology
- 2008
- 287
- PDF
Sigma receptors: potential targets for a new class of antidepressant drug.
- Medicine
- Pharmacology & therapeutics
- 2010
- 99
Met5‐enkephalin‐Arg 6‐Phe7, an endogenous neuropeptide, binds to multiple opioid and nonopioid sites in rat brain
- Chemistry, Medicine
- Journal of neuroscience research
- 1997
- 79
Uniform assessment and ranking of opioid μ receptor binding constants for selected opioid drugs.
- Chemistry, Medicine
- Regulatory toxicology and pharmacology : RTP
- 2011
- 200
- PDF
Structural Insights into σ1 Receptor Interactions with Opioid Ligands by Molecular Dynamics Simulations
- Chemistry, Medicine
- Molecules
- 2018
- 1
- PDF
Ether modifications to 1-[2-(3,4-dimethoxyphenyl)ethyl]-4-(3-phenylpropyl)piperazine (SA4503): effects on binding affinity and selectivity for sigma receptors and monoamine transporters.
- Chemistry, Medicine
- Bioorganic & medicinal chemistry
- 2015
- 7