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2011, BMC Pharmacology
Journal of medicinal chemistry
Synthesis and pharmacological evaluation of aminothiazolomorphinans at the mu and kappa opioid receptors2013 •
Previous studies with aminothiazolomorphinans suggested that this class of opioid ligands may be useful as a potential pharmacotherapeutic to decrease drug abuse. Novel aminothiazole derivatives of cyclorphan were prepared to evaluate a series of aminothiazolomorphinans with varying pharmacological properties at the κ opioid receptor (KOR) and μ opioid receptor (MOR). This study was focused on exploring the regioisomeric analogs with the aminothiazole on the C-ring of the morphinan skeleton. Receptor binding and [(35)S]GTPγS binding assays were used to characterize the affinity and pharmacological properties of the aminothiazolomorphinans. Intracranial self-stimulation (ICSS) was used to compare the effects of a representative aminothiazolomorphinan with the morphinan mixed-KOR/MOR agonist butorphan (MCL-101) on brain-stimulation reward.
Bioorganic & Medicinal Chemistry
In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors2007 •
Journal of Medicinal Chemistry
Synthesis, Binding Affinity, and Functional in Vitro Activity of 3-Benzylaminomorphinan and 3-Benzylaminomorphine Ligands at Opioid Receptors2012 •
Journal of Medicinal Chemistry
Synthesis and Opioid Receptor Binding Affinities of 2-Substituted and 3-Aminomorphinans: Ligands for μ, κ, and δ Opioid Receptors2010 •
Journal of Medicinal Chemistry
Identification of Opioid Ligands Possessing Mixed μ Agonist/δ Antagonist Activity among Pyridomorphinans Derived from Naloxone, Oxymorphone, and Hydromorphone2004 •
Scientific Reports
N-Phenethyl Substitution in 14-Methoxy-N-methylmorphinan-6-ones Turns Selective µ Opioid Receptor Ligands into Dual µ/δ Opioid Receptor AgonistsMorphine and structurally-derived compounds are µ opioid receptor (µOR) agonists, and the most effective analgesic drugs. However, their usefulness is limited by serious side effects, including dependence and abuse potential. The N-substituent in morphinans plays an important role in opioid activities in vitro and in vivo. This study presents the synthesis and pharmacological evaluation of new N-phenethyl substituted 14-O-methylmorphinan-6-ones. Whereas substitution of the N-methyl substituent in morphine (1) and oxymorphone (2) by an N-phenethyl group enhances binding affinity, selectivity and agonist potency at the µOR of 1a and 2a, the N-phenethyl substitution in 14-methoxy-N-methylmorphinan-6-ones (3 and 4) converts selective µOR ligands into dual µ/δOR agonists (3a and 4a). Contrary to N-methylmorphinans 1–4, the N-phenethyl substituted morphinans 1a–4a produce effective and potent antinociception without motor impairment in mice. Using docking and molecular dynamics simulation...
2014 •
Bioorganic & Medicinal Chemistry
Synthesis and binding affinity of novel mono- and bivalent morphinan ligands for κ, μ, and δ opioid receptors2011 •
Life Sciences
Opioid binding profiles of new hydrazone, oxime, carbazone and semicarbazone derivatives of 14-alkoxymorphinans1999 •
Journal of Medicinal Chemistry
Synthesis, Pharmacology, and Molecular Docking Studies on 6-Desoxo-N-methylmorphinans as Potent μ-Opioid Receptor Agonists2017 •
Position 6 of the morphinan skeleton plays a key role in the μ-opioid receptor (MOR) activity in vitro and in vivo. We describe the consequence of the 6-carbonyl group deletion in N-methylmorphinan-6-ones 1−4 on ligand−MOR interaction, signaling, and antinociception. While 6-desoxo compounds 1a, 2a, and 4a show similar profiles to their 6-keto counterparts, the 6-desoxo-14-benzyloxy substituted 3a displays significantly increased MOR binding and agonist potency and a distinct binding mode compared with its analogue 3.
Archäologische Denkmalpflege 4
Deutschlands Archäologie zwischen Gemeinfreiheit und Umsatzsteuer2024 •
Наукові зошити історичного факультету Львівського університету, 24
“ВИПРАВИТИ ПОМИЛКИ, КЕРУЮЧИ ДЕРЖАВОЮ З УСІЄЮ СТАРАННІСТЮ”: АВАРСЬКА ПОЛІТИКА ТИБЕРІЯ ІІ КОНСТЯНТИНА (578–582) [“CORRECT MY MISTAKES BY GOVERNING THE STATE WITH ALL ZEAL”: THE AVARIAN POLICY OF TIBERIUS II CONSTANTINE (578–582)]2023 •
Revista Heródoto - Revista do Grupo de Estudos e Pesquisas sobre a Antiguidade Clássica e suas conexões Afro-Asiáticas
A Casa Fenício-Púnica2017 •
Animal Production Science
Crambe cake impairs lamb performance and fatty acid profile of meat2017 •
Journal of Biomechanics
Cervical spine mechanics as a function of transection of components1975 •
2019 •
Pakistan Journal of Medical and Health Sciences
Did We Deliver Quality Education in Online Sessions During Covid 19 Lock Down? Learner’s Perspective from a Developing CountryCOLLOQUIUM HUMANARUM
Ser Professor No Século XXI: As Representações Sociais De Alunos Ingressantes e Concluintes De Um Curso De Pedagogia2016 •
2013 •
Jurnal Ilmu dan Teknologi Peternakan Tropis
MUTU DAGING SAPI BALI YANG DIMARINASI DALAM JUS BUAH PINANG (Areca catechu L.) DENGAN KONSENTRASI YANG BERBEDA2017 •