Results 81 to 90 of about 400 (115)

The c-Src inhibitor eCF506 diminishes opioid tolerance creating bias against β-arrestin2 recruitment

open access: yes
Singleton S   +6 more
europepmc   +1 more source

Identification of Spiro[chromene-2,4'-piperidine]s as Potent, Selective, and Gq-Biased 5-HT2C Receptor Partial Agonists. [PDF]

open access: yesACS Med Chem Lett
Jiang G   +8 more
europepmc   +1 more source

Rational Design Biased Compounds against μ‑Opioid Receptor. [PDF]

open access: yesACS Pharmacol Transl Sci
Wu C, Li Y, Vogel H, Yuan S.
europepmc   +1 more source

Biased agonism of clinically approved μ-opioid receptor agonists and TRV130 is not controlled by binding and signaling kinetics

open access: yesNeuropharmacology, 2020
Binding and signaling kinetics have previously proven important in validation of biased agonism at GPCRs. Here we provide a comprehensive kinetic pharmacological comparison of clinically relevant μ-opioid receptor agonists, including the novel biased agonist oliceridine (TRV130) which is in clinical trial for pain management.
Emil Marcher-Rørsted   +2 more
exaly   +6 more sources

Approval of oliceridine (TRV130) for intravenous use in moderate to severe pain in adults [PDF]

open access: yesBritish Journal of Anaesthesia, 2020
EditordOpioids used for the treatment of moderate to severe pain in an appropriate setting with appropriate management (stewardship) have good efficacy. However, when these are used long term their efficacy is questionable. Tolerance develops leading to escalating doses and a vicious circle of side-effects.
David G Lambert, Girolamo Calò
exaly   +5 more sources

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