The utilization of mu-opioid receptor biased agonists: oliceridine, an opioid analgesic with reduced adverse effects
Abstract Purpose of Review The purpose of this review is to summarize the current
understanding of opioid pathways in mediating and/or modulating analgesia and adverse …
understanding of opioid pathways in mediating and/or modulating analgesia and adverse …
The potent opioid agonist,(+)-cis-3-methylfentanyl binds pseudoirreversibly to the opioid receptor complex in vitro and in vivo: evidence for a novel mechanism of …
The present study demonstrates that pretreatment of rat brain membranes with (+)-cis-3-
methylfentanyl {(+)-cis-MF}, followed by extensive washing of the membranes, produces a …
methylfentanyl {(+)-cis-MF}, followed by extensive washing of the membranes, produces a …
[HTML][HTML] The rising crisis of illicit fentanyl use, overdose, and potential therapeutic strategies
Y Han, W Yan, Y Zheng, MZ Khan, K Yuan… - Translational psychiatry, 2019 - nature.com
Fentanyl is a powerful opioid anesthetic and analgesic, the use of which has caused an
increasing public health threat in the United States and elsewhere. Fentanyl was initially …
increasing public health threat in the United States and elsewhere. Fentanyl was initially …
[HTML][HTML] Naloxone's dose-dependent displacement of [11C]carfentanil and duration of receptor occupancy in the rat brain
Y Kang, KA O'Conor, AC Kelleher, J Ramsey… - Scientific reports, 2022 - nature.com
The continuous rise in opioid overdoses in the United States is predominantly driven by very
potent synthetic opioids, mostly fentanyl and its derivatives (fentanyls). Although naloxone …
potent synthetic opioids, mostly fentanyl and its derivatives (fentanyls). Although naloxone …
[HTML][HTML] Pharmacological investigations of N-substituent variation in morphine and oxymorphone: opioid receptor binding, signaling and antinociceptive activity
Morphine and structurally related derivatives are highly effective analgesics, and the
mainstay in the medical management of moderate to severe pain. Pharmacological actions …
mainstay in the medical management of moderate to severe pain. Pharmacological actions …
Sensitization and tolerance to the discriminative stimulus effects of mu-opioid agonists
CA Paronis, SG Holtzman - Psychopharmacology, 1994 - Springer
The discriminative stimulus effects of several μ-opioid agonists were examined under
conditions of opioid sensitization or tolerance, ie, before and after 1-week SC infusions of …
conditions of opioid sensitization or tolerance, ie, before and after 1-week SC infusions of …
Synthesis and evaluation of 1-and 2-substituted fentanyl analogs for opioid activity
MYH Essawi, PS Portoghese - Journal of medicinal chemistry, 1983 - ACS Publications
We synthesized fentanyl analogues that possess key groups common to theopioid peptides
to investigate whether or not these two classes of compounds interact with common subsites …
to investigate whether or not these two classes of compounds interact with common subsites …
Phenethyl-4-ANPP: a marginally active byproduct suggesting a switch in illicit fentanyl synthesis routes
Profiling of the illicit fentanyl supply is invaluable from surveillance and intelligence
perspectives. An important strategy includes the study of chemical attribution signatures (eg …
perspectives. An important strategy includes the study of chemical attribution signatures (eg …
Selective enhancement of fentanyl-induced antinociception by the delta agonist SNC162 but not by ketamine in rhesus monkeys: further evidence supportive of delta …
ML Banks, JE Folk, KC Rice, SS Negus - Pharmacology Biochemistry and …, 2010 - Elsevier
Mu-opioid receptor agonists such as fentanyl are effective analgesics, but their clinical use is
limited by untoward effects. Adjunct medications may improve the effectiveness and/or safety …
limited by untoward effects. Adjunct medications may improve the effectiveness and/or safety …
[HTML][HTML] How μ-opioid receptor recognizes fentanyl
Roughly half of the drug overdose-related deaths in the United States are related to
synthetic opioids represented by fentanyl which is a potent agonist of mu-opioid receptor …
synthetic opioids represented by fentanyl which is a potent agonist of mu-opioid receptor …