New μ-Opioid Receptor Agonists with Piperazine Moiety

New μ-Opioid Receptor Agonists with Piperazine Moiety

New μ-opioid receptor (MOR) agonists containing piperazine and homopiperazine moieties in the structures were synthesized and their affinities to and agonist potencies on MOR were evaluated. Among the synthesized compounds, 4-[4-(2-methoxyphenyl)piperazin-1-yl]-N,N-dimethyl-2,2-diphenylbutanamide (2...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Veröffentlicht in:Chemical & pharmaceutical bulletin 2001, Vol.49(10), pp.1314-1320
Hauptverfasser: KOMOTO, Teruo, OKADA, Tomomi, SATO, Susumu, NIINO, Yasuhiro, OKA, Tetsuo, SAKAMOTO, Takao
Format: Artikel
Sprache:eng
Schlagworte:
Animals
Biological and medical sciences
CHO Cells
Cricetinae
cross-coupling
Enkephalin, Ala-MePhe-Gly- - pharmacology
Guinea Pigs
Humans
Ileum - drug effects
In Vitro Techniques
Indicators and Reagents
Magnetic Resonance Spectroscopy
Male
Mass Spectrometry
Medical sciences
Muscle, Smooth - drug effects
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Pd-catalyzed amination
Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems
Pharmacology. Drug treatments
piperazine
Piperazines - chemical synthesis
Piperazines - chemistry
Piperazines - pharmacology
Receptors, Opioid, kappa - antagonists & inhibitors
Receptors, Opioid, mu - agonists
Spectrophotometry, Infrared
μ-opioid receptor agonist
Online-Zugang:Volltext
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:New μ-opioid receptor (MOR) agonists containing piperazine and homopiperazine moieties in the structures were synthesized and their affinities to and agonist potencies on MOR were evaluated. Among the synthesized compounds, 4-[4-(2-methoxyphenyl)piperazin-1-yl]-N,N-dimethyl-2,2-diphenylbutanamide (20Aa) showed the highest affinity to the human MOR expressed in Chinese hamster ovary (CHO)-K1 cells, and the highest agonist potency on the MOR in isolated guinea-pig ileum preparation.
ISSN:0009-2363
1347-5223
DOI:10.1248/cpb.49.1314