LPA3: Pharmacodynamic Differences Between Lysophosphatidic Acid and Oleoyl-Methoxy Glycerophosphothionate: Biased Agonism, Two Sites

Authors: K. Helivier Solís, M. Teresa Romero-Ávila, Ruth Rincón-Heredia, Juan Carlos Martínez-Morales, J. Adolfo García-Sáinz

Source: Receptors, Vol 3, Iss 4, Pp 555-573 (2024)

Subject Terms: lysophosphatidic acid, LPA, LPA3 receptor, oleoyl-methoxy glycerophosphothionate, OMPT, biased agonism, Genetics, QH426-470, Physical and theoretical chemistry, QD450-801

File Description: electronic resource

Relation: https://www.mdpi.com/2813-2564/3/4/29; https://doaj.org/toc/2813-2564

Access URL: https://doaj.org/article/58dc5a4f7b0f49248c046154d41c2074

Global Trends in Oliceridine (TRV130) Research from 2013 to 2024: A Bibliometrics and Knowledge Graph Analysis

Authors: Wang C, Liu L, Bai X

Source: Drug Design, Development and Therapy, Vol Volume 18, Pp 4681-4692 (2024)

Subject Terms: opioid receptors, biased agonism, oliceridine, bibliometrics, Therapeutics. Pharmacology, RM1-950

File Description: electronic resource

Relation: https://www.dovepress.com/global-trends-in-oliceridine-trv130-research-from-2013-to-2024-a-bibli-peer-reviewed-fulltext-article-DDDT; https://doaj.org/toc/1177-8881

Access URL: https://doaj.org/article/f1b15d16941441eab92581ea11cd536e

Attributes novel drug candidate: Constitutive GPCR signal bias mediated by purinergic receptors

Authors: Yin, Li ^{a, 1}, Ni, Kexin ^{a, 1}, Mao, Tianqi ^{b, 1}, Tian, Sheng ^{b, ⁎}, Liu, Chunxiao ^c, Chen, Jiayao ^a, Zhou, Mengze ^{a, ⁎⁎}, Li, Huanqiu ^{b, ⁎}, Hu, Qinghua ^{a, c, ⁎⁎}

Source: In Pharmacology and Therapeutics March 2025 267

Biased agonism at free-fatty acid receptor-4 (FFA4/GPR120)

Authors: Teyani, Razan L. ^a, Moniri, Nader H. ^{a, b, ⁎}

Source: In Pharmacology and Therapeutics February 2025 266

Oxytocin receptors within the caudal lateral septum regulate social approach-avoidance, long-term social discrimination, and anxiety-like behaviors in adult male and female rats

Authors: Pirri, Fardad ^a, McCormick, Cheryl M. ^{a, b, ⁎}

Source: In Neuropharmacology 15 June 2025 271

Biased agonism in peptide-GPCRs: A structural perspective

Authors: Jayakody, Tharindunee ^a, Budagoda, Dinath Kavishka ^a, Mendis, Krishan ^a, Dilshan, Withanage Dhanuka ^a, Bethmage, Duvindu ^a, Dissasekara, Rashmi ^{a, f}, Dawe, Gavin Stewart ^{b, c, d, e, ⁎}

Source: In Pharmacology and Therapeutics May 2025 269

Effects of Biased Analogues of the Kappa Opioid Receptor Agonist, U50,488, in Preclinical Models of Pain and Side Effects

Authors: Ross van de Wetering, Loan Y. Vu, Lindsay D. Kornberger, Dan Luo, Brittany Scouller, Sheein Hong, Kelly Paton, Thomas E. Prisinzano, Bronwyn M. Kivell

Source: Molecules, Vol 30, Iss 3, p 604 (2025)

Subject Terms: kappa opioid receptor, anti-nociception, pain, side effects, biased agonism, signaling bias, Organic chemistry, QD241-441

File Description: electronic resource

Relation: https://www.mdpi.com/1420-3049/30/3/604; https://doaj.org/toc/1420-3049

Access URL: https://doaj.org/article/17f2c31cf3714c52a18c44781bc0f6da

Receptor activity-modifying protein modulation of parathyroid hormone-1 receptor function and signaling

Authors: Paris Avgoustou, Ameera B. A. Jailani, Aditya J. Desai, David J. Roberts, Ewan R. Lilley, Grant W. Stothard, Timothy M. Skerry, Gareth O. Richards

Source: Frontiers in Pharmacology, Vol 15 (2024)

Subject Terms: parathyroid hormone receptor-1, parathyroid hormone, parathyroid hormone-related protein, receptor-activity-modifying protein, biased agonism, Therapeutics. Pharmacology, RM1-950

File Description: electronic resource

Relation: https://www.frontiersin.org/articles/10.3389/fphar.2024.1455231/full; https://doaj.org/toc/1663-9812

Access URL: https://doaj.org/article/1234b7238d294ca4875ee9bfc9802527

Oliceridine for the Management of Moderate to Severe Acute Postoperative Pain: A Narrative Review

Authors: Daksla N, Wang A, Jin Z, Gupta A, Bergese SD

Source: Drug Design, Development and Therapy, Vol Volume 17, Pp 875-886 (2023)

Subject Terms: postoperative pain, opioids, multimodal analgesia, opioid-related adverse events, biased agonism, Therapeutics. Pharmacology, RM1-950

File Description: electronic resource

Relation: https://www.dovepress.com/oliceridine-for-the-management-of-moderate-to-severe-acute-postoperati-peer-reviewed-fulltext-article-DDDT; https://doaj.org/toc/1177-8881

Access URL: https://doaj.org/article/4ae4d7939d3744ff83bc41f4c182ab5a

Quantitative receptor model for responses that are left- or right-shifted versus occupancy (are more or less concentration sensitive): the SABRE approach

Authors: Peter Buchwald

Source: Frontiers in Pharmacology, Vol 14 (2023)

Subject Terms: affinity, biased agonism, efficacy, G-protein coupled receptors, ligand binding, opioid receptor, Therapeutics. Pharmacology, RM1-950

File Description: electronic resource

Relation: https://www.frontiersin.org/articles/10.3389/fphar.2023.1274065/full; https://doaj.org/toc/1663-9812

Access URL: https://doaj.org/article/6a4d0370f515439581abe98e0c0430ae

ClickArr: a novel, high-throughput assay for evaluating β-arrestin isoform recruitment

Authors: Alexander R. French, Yazan J. Meqbil, Richard M. van Rijn

Source: Frontiers in Pharmacology, Vol 14 (2023)

Subject Terms: G protein–coupled receptors, biased agonism, delta opioid receptor, high-throughput drug screen, click beetle luciferase, signal transduction, Therapeutics. Pharmacology, RM1-950

File Description: electronic resource

Relation: https://www.frontiersin.org/articles/10.3389/fphar.2023.1295518/full; https://doaj.org/toc/1663-9812

Access URL: https://doaj.org/article/226cef4e1ff64cb6bf6f37cbbe6fe9e4

Fingerprinting heterocellular β-adrenoceptor functional expression in the brain using agonist activity profiles

Authors: Rachel A. Matt, Frederick G. Westhorpe, Rosemary F. Romuar, Payal Rana, Joel R. Gever, Anthony P. Ford

Source: Frontiers in Molecular Biosciences, Vol 10 (2023)

Subject Terms: adrenergic, noradrenergic, GPCR, biased agonism, agonist, desensitization, Biology (General), QH301-705.5

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Relation: https://www.frontiersin.org/articles/10.3389/fmolb.2023.1214102/full; https://doaj.org/toc/2296-889X

Access URL: https://doaj.org/article/34a4c0f376f345a38da1a4da5f3b6f14

The AT1/AT2 Receptor Equilibrium Is a Cornerstone of the Regulation of the Renin Angiotensin System beyond the Cardiovascular System

Authors: Mélissa Colin, Céline Delaitre, Sébastien Foulquier, François Dupuis

Source: Molecules, Vol 28, Iss 14, p 5481 (2023)

Subject Terms: AT1 receptor, AT2 receptor, angiotensin II, AT1/AT2 balance, biased agonism, TRV120027, Organic chemistry, QD241-441

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Relation: https://www.mdpi.com/1420-3049/28/14/5481; https://doaj.org/toc/1420-3049

Access URL: https://doaj.org/article/63886a0e668f4b4a8069a94875b95e26

Opioids and Their Receptors

Contributors: Spetea, Mariana, Schmidhammer, Helmut

Subject Terms: opioid receptors, neurokinin-1 receptor, peptide synthesis, receptor binding studies, functional assay, writhing test, tolerance, Leu-enkephalin, beta-arrestin, mu opioid receptor, delta opioid receptor, biased signaling, DADLE, ischemia, plasma stability, morphinan, BNTX, δ opioid receptor antagonist, 1H-NMR experiments, mechanism elucidation, peripheral antinociception, 14-methoxycodeine-6-O-sulfate, codeine-6-O-sulfate, opioid peptides and peptidomimetics, DAMGO, DALDA, [Dmt1]DALDA, KGOP01, binding, molecular docking, structure-activity relationships, β2-amino acids, β2-Homo-amino acids, µ-opioid receptor, opioid peptides, TAPP, racemic synthesis of β2-amino acids, peripheral µ-opioid receptors, analgesia, peripheral analgesic tolerance, dysbiosis, opioid, bifunctional ligands, (−)-N-phenethylnorhydromorphone analogs, [35S]GTPgammaS assay, forskolin-induced cAMP accumulation assays, β-arrestin recruitment assays, MOR and DOR agonists, respiratory depression, bias factor, molecular modeling &, simulation, δ opioid receptor, NTI derivative, sulfonamide, inverse agonist, neutral antagonist, agonist, opioids, mu receptor, opioid side effects, biased agonism, partial agonism, zerumbone, chronic constriction injury (CCI), allodynia, hyperalgesia, potassium channels, over-the-counter drugs, misuse, abuse, opioid drugs, pharmacology, codeine, dihydrocodeine, loperamide, opioid peptide, macrocyclic tetrapeptide, multifunctional ligands, kappa opioid receptor, analgesics, opioid liabilities, μ opioid receptor, receptor model, biased ligands, dependence, pain therapy, neonatal opioid withdrawal syndrome, naltrexone, 6β-naltrexol, buprenorphine, G-protein bias, arrestin recruitment, respiration, mitragynine, heteromer, internalization, primary hippocampal culture, lysosomes, µ opioid receptor, molecular dynamics, docking, interaction fingerprints, biased agonists, SR-17018, PZM21, morphine, fentanyl, diphenethylamines, design and synthesis, structure–activity relationships, partial agonist, biased agonist, antagonist, binding affinity, selectivity, Medicine and Nursing

File Description: application/octet-stream

Access URL: https://directory.doabooks.org/handle/20.500.12854/69428
https://mdpi.com/books/pdfview/book/3230

Editorial: Kappa opioid receptors revealed: Disentangling the pharmacology to open up new therapeutic strategies

Authors: Wendy Margaret Walwyn, Marta Valenza

Source: Frontiers in Pharmacology, Vol 13 (2022)

Subject Terms: addiction, biased agonism, dynorphins, G-protein, Kappa opioid receptor OR KOR OR KOPr OR KOP, opioids, Therapeutics. Pharmacology, RM1-950

File Description: electronic resource

Relation: https://www.frontiersin.org/articles/10.3389/fphar.2022.973780/full; https://doaj.org/toc/1663-9812

Access URL: https://doaj.org/article/7040afbef9ad47ac9c325cf2c730c31c

Dose-Dependent Regulation on Prefrontal Neuronal Working Memory by Dopamine D1 Agonists: Evidence of Receptor Functional Selectivity-Related Mechanisms

Authors: Yang Yang, Susan D. Kocher, Mechelle M. Lewis, Richard B. Mailman

Source: Frontiers in Neuroscience, Vol 16 (2022)

Subject Terms: dopamine D1 agonist, dose response analysis, prefrontal cortex, working memory, functional selectivity/biased agonism, Neurosciences. Biological psychiatry. Neuropsychiatry, RC321-571

File Description: electronic resource

Relation: https://www.frontiersin.org/articles/10.3389/fnins.2022.898051/full; https://doaj.org/toc/1662-453X

Access URL: https://doaj.org/article/a9042f49303c4ceaa7f3708169473a6c

Pharmacology of Kappa Opioid Receptors: Novel Assays and Ligands

Authors: Chiara Sturaro, Davide Malfacini, Michela Argentieri, Francine M. Djeujo, Erika Marzola, Valentina Albanese, Chiara Ruzza, Remo Guerrini, Girolamo Calo’, Paola Molinari

Source: Frontiers in Pharmacology, Vol 13 (2022)

Subject Terms: kappa opioid receptor, G protein-coupled receptor, label-free, BRET, calcium mobilization, biased agonism, Therapeutics. Pharmacology, RM1-950

File Description: electronic resource

Relation: https://www.frontiersin.org/articles/10.3389/fphar.2022.873082/full; https://doaj.org/toc/1663-9812

Access URL: https://doaj.org/article/25d09c7909904b40bb5b128ded4d84b3

Hyperactivity in Mice Induced by Opioid Agonists with Partial Intrinsic Efficacy and Biased Agonism Administered Alone and in Combination with Morphine

Authors: Agnes Acevedo-Canabal, Travis W. Grim, Cullen L. Schmid, Nina McFague, Edward L. Stahl, Nicole M. Kennedy, Thomas D. Bannister, Laura M. Bohn

Source: Biomolecules, Vol 13, Iss 6, p 935 (2023)

Subject Terms: GPCR, biased agonism, oliceridine, partial agonist, striatum, SR-17018, Microbiology, QR1-502

File Description: electronic resource

Relation: https://www.mdpi.com/2218-273X/13/6/935; https://doaj.org/toc/2218-273X

Access URL: https://doaj.org/article/14dc2c96072240f297e8663c127868ee

An updated assessment of the translational promise of G-protein-biased kappa opioid receptor agonists to treat pain and other indications without debilitating adverse effects

Authors: Alexander R. French, Richard M. van Rijn

Source: Pharmacological Research, Vol 177, Iss , Pp 106091- (2022)

Subject Terms: Kappa opioid receptor, Biased agonism, Antinociception, Aversion, Sedation, Depression, Therapeutics. Pharmacology, RM1-950

File Description: electronic resource

Relation: http://www.sciencedirect.com/science/article/pii/S1043661822000366; https://doaj.org/toc/1096-1186

Access URL: https://doaj.org/article/f4cae45bd8d543e78f83cd7f482312fd

The Binding Mode to Orthosteric Sites and/or Exosites Underlies the Therapeutic Potential of Drugs Targeting Cannabinoid CB2 Receptors

Authors: Rafael Franco, Paula Morales, Gemma Navarro, Nadine Jagerovic, Irene Reyes-Resina

Source: Frontiers in Pharmacology, Vol 13 (2022)

Subject Terms: biased agonism, heteromer, health benefits, therapy, functional selectivity, cannabinoid receptor, Therapeutics. Pharmacology, RM1-950

File Description: electronic resource

Relation: https://www.frontiersin.org/articles/10.3389/fphar.2022.852631/full; https://doaj.org/toc/1663-9812

Access URL: https://doaj.org/article/afbbc5a71e5e4873b7b89ddbc373f385