Abstract
A series of N-biarylalkyl-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-ones were prepared and evaluated for biological activity at opioid (μ, δ, κ) and opioid receptor like-1 (ORL-1) G-protein coupled receptors. Substitution on the biaryl moiety produced enhanced affinity for the μ-opioid receptor.
Keywords: mu receptor, delta receptor, kappa receptor, nociceptin receptor, pain, 1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one, heteroarylphenylalkyl, sar, [35s]gtpγs binding assay, suzuki reaction
Medicinal Chemistry
Title: 8-(Heteroaryl)phenalkyl-1-Phenyl-1,3,8-triazaspiro[4.5]decan-4-ones as Opioid Receptor Modulators
Volume: 1 Issue: 6
Author(s): A. D. Jordan, M. J. Orsini, S. A. Middleton, P. J. Connolly, D. E. Brenneman, K. Pan and A. B. Reitz
Affiliation:
Keywords: mu receptor, delta receptor, kappa receptor, nociceptin receptor, pain, 1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one, heteroarylphenylalkyl, sar, [35s]gtpγs binding assay, suzuki reaction
Abstract: A series of N-biarylalkyl-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-ones were prepared and evaluated for biological activity at opioid (μ, δ, κ) and opioid receptor like-1 (ORL-1) G-protein coupled receptors. Substitution on the biaryl moiety produced enhanced affinity for the μ-opioid receptor.
Export Options
About this article
Cite this article as:
Jordan D. A., Orsini J. M., Middleton A. S., Connolly J. P., Brenneman E. D., Pan K. and Reitz B. A., 8-(Heteroaryl)phenalkyl-1-Phenyl-1,3,8-triazaspiro[4.5]decan-4-ones as Opioid Receptor Modulators, Medicinal Chemistry 2005; 1 (6) . https://dx.doi.org/10.2174/157340605774598207
DOI https://dx.doi.org/10.2174/157340605774598207 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Editorial (Thematic Issue: Targeting Phosphodiesterases (PDEs) for Treatment of CNS Diseases)
Current Pharmaceutical Design Deciphering the Role of Aberrant Protein Post-Translational Modification in the Pathology of Neurodegeneration
CNS & Neurological Disorders - Drug Targets Fumaric Acid and its Esters: An Emerging Treatment for Multiple Sclerosis
Current Neuropharmacology Retrograde Modulation of Synaptic Transmission Mediated by Endogenous Cannabinoids
Current Neuropharmacology Exercise-Induced Cardiac Troponin Release: Real-Life Clinical Confusion
Current Medicinal Chemistry Lesions and Dysfunctions of the Nucleus Basalis as Alzheimers Disease Models: General and Critical Overview and Analysis of the Long-Term Changes in Several Excitotoxic Models
Current Alzheimer Research Lower K<sub>V</sub>7.5 Potassium Channel Subunit Expression in an Animal Model of Paroxysmal Dystonia
CNS & Neurological Disorders - Drug Targets Adenosine and the Auditory System
Current Neuropharmacology Update in Pharmacological Management of Coronary No-Reflow Phenomenon
Cardiovascular & Hematological Agents in Medicinal Chemistry Delivery and Application of Dietary Polyphenols to Target Organs, Tissues and Intracellular Organelles
Current Drug Metabolism Commentary (Research Highlights)
CNS & Neurological Disorders - Drug Targets Bioactive Compounds in Some Culinary Aromatic Herbs and Their Effects on Human Health
Mini-Reviews in Medicinal Chemistry Recent Development in Liquid Chromatography/Mass Spectrometry and Emerging Technologies for Metabolite Identification
Current Drug Metabolism Inhaled Biologics: From Preclinical to Product Approval
Current Pharmaceutical Design Anti-IgE Therapy with Omalizumab for Severe Asthma: Current Concepts and Potential Developments
Current Drug Targets Development, Potential Anticancer Activity and the Receptor Profile of Different Functionalized 1,3,5-Triazine Derivatives
Mini-Reviews in Medicinal Chemistry Regulation of Neurogenesis and Gliogenesis by Stress and Antidepressant Treatment
CNS & Neurological Disorders - Drug Targets Lipid-Based Nanoparticulate Systems for the Delivery of Anti-Cancer Drug Cocktails: Implications on Pharmacokinetics and Drug Toxicities
Current Drug Metabolism Editorial (Thematic Issue: Impact of Early Life Stress on Psychiatric Disorders: Searching New Biomarkers and Innovative Pharmacological Targets)
Current Pharmaceutical Design Animal Models for Investigating Benign Essential Blepharospasm
Current Neuropharmacology