TRV130 inhibits colon cancer progression via suppressing the Hedgehog signaling pathway: in vitro and in vivo evidence [PDF]
HereditasBackground Colon cancer, characterized by high incidence and mortality, faces clinical challenges due to high recurrence rates and drug resistance. Aberrant activation of Hedgehog (Hh) signaling pathway is a key driver of colon cancer progression, making
Yuanzhao Zhuang +3 more
exaly +6 more sources
Global Trends in Oliceridine (TRV130) Research from 2013 to 2024: A Bibliometrics and Knowledge Graph Analysis [PDF]
Drug Design, Development and TherapyCong Wang,1 Lidan Liu,1 Xue Bai2 1Department of Anesthesiology, Shengjing Hospital of China Medical University, Shenyang, Liaoning Province, People’s Republic of China; 2Department of Health Management, Shengjing Hospital of China Medical University ...
Wang C, Liu L, Bai X
doaj +4 more sources
TRV130 partial agonism and capacity to induce anti‐nociceptive tolerance revealed through reducing available μ‐opioid receptor number [PDF]
British Journal of Pharmacology, 2021 Background and Purpose β‐Arrestin2 recruitment to μ‐receptors may contribute to the development of opioid side effects. This possibility led to the development of TRV130 and PZM21, opioids reportedly biased against β‐arrestin2 recruitment in favour of G‐protein signalling.
Daniel T Baptista-Hon, Tim G Hales
exaly +5 more sources
Effect of TRV130 and methadone on fentanyl-vs.-food choice and somatic withdrawal signs in opioid-dependent and post-opioid-dependent rats [PDF]
Neuropsychopharmacology, 2022 The high efficacy mu-opioid receptor (MOR) agonist methadone is an effective opioid use disorder (OUD) medication used exclusively in opioid-dependent patients. However, methadone has undesirable effects that limit its clinical efficacy. Intermediate efficacy MOR agonists may treat OUD with fewer undesirable effects.
E Andrew Townsend +2 more
exaly +4 more sources
Biased Opioid Ligands: Revolution or Evolution? [PDF]
Frontiers in Pain Research, 2021 Opioid are the most powerful analgesics ever but their use is still limited by deleterious side effects such as tolerance, dependence, and respiratory depression that could eventually lead to a fatal overdose. The opioid crisis, mainly occurring in north
Florence Noble, Nicolas Marie
doaj +2 more sources
A Comparison of Oliceridine versus Sufentanil for Patient-Controlled Analgesia After Total Knee Arthroplasty in Elderly Patients: A Double-Blinded Randomized Controlled Study [PDF]
Drug Design, Development and TherapyXi Liu,1,* Suna Wang,2,* Xiaoxiao Chen,1,* Yuanyuan Tian,1 Junli Sun,1 Aizhong Wang,1 Qi Li,1 Hui Zhang1 1Department of Anesthesiology, Shanghai Sixth People’s Hospital Affiliated with Shanghai Jiao Tong University School of ...
Liu X +7 more
doaj +2 more sources
Nausea and vomiting as adverse events of oliceridine: a systematic review and meta-analysis of randomized controlled trials [PDF]
Frontiers in PharmacologyBackgroundPostoperative nausea and vomiting (PONV) continue to be some of the most common and troublesome complications following anesthesia. Oliceridine, a G protein-biased µ-opioid receptor agonist, has the potential to provide effective pain relief ...
Jinfang Zeng +4 more
doaj +2 more sources
MedComm, Volume 3, Issue 3, September 2022., 2022 1. Rewarding effects and withdrawal syndrome are two dominant components of opioid addiction. 2. Mu‐opioid receptors (MORs) are highly involved in reward circuitry and the development of withdrawal syndrome. 3. MORs are important targets to treat addiction and withdrawal syndrome.
Jia‐Jia Zhang +5 more
wiley +1 more source
Strukturbasierte Entwicklung von G‐Protein bevorzugenden μ‐Opioidrezeptor Agonisten
Angewandte Chemie, Volume 134, Issue 26, June 27, 2022., 2022 Wir haben Kryo‐EM‐Strukturen des μ‐Opioidrezeptors (μOR), in Komplex mit der Leitsubstanz PZM21 und dem neu entwickelten Agonisten FH210 bestimmt, um den Mechanismus ihrer funktionellen Selektivität zu verstehen und die Entwicklung von Analgetika der nächsten Generation mit weniger Nebenwirkungen voranzutreiben.
Haoqing Wang +9 more
wiley +1 more source
Structure‐Based Evolution of G Protein‐Biased μ‐Opioid Receptor Agonists
Angewandte Chemie International Edition, Volume 61, Issue 26, June 27, 2022., 2022 cryoEM structures of the μ‐opioid receptor (μOR) bound to the lead compound PZM21 and the newly developed agonist FH210 were obtained to understand the mechanism of their biased signaling and to guide the evolution of next‐generation analgesics with fewer adverse effects.
Haoqing Wang +9 more
wiley +1 more source