Results 81 to 90 of about 729,259 (302)

Cannabinoid CB1 Receptor in Nociceptors Mediates Postoperative Analgesia via ASIC3 Inhibition

Advanced Science, EarlyView.
CB1R and ASIC3 are co‐expressed in CGRP+ nociceptors of mouse DRG. Plantar incision triggers an upregulation of ASIC3 and activation of ASIC3+ neurons, driving mechanical allodynia. CB1R activation suppresses ASIC3 function and downstream ERK1/2 phosphorylation, thereby braking nociceptive signaling and accelerating pain resolution.
Kangtai Xu, Luyao Ji, Haoyi Yang, Xiying Chen, Qiaodan Hu, Haimei He, Jiawei Wu, Leyan Shan, Shihui Feng, Yingzhi Li, Xiongchang Tan, Hao Wang, Zilong Wang, Chaoran Wu   +13 more
wiley   +1 more source

Beyond Nature's Blueprint: Macrocyclic Peptides Containing Unnatural Amino Acids in Therapeutic Development

Angewandte Chemie, EarlyView.
Strategic incorporation of unnatural amino acids transforms macrocyclic peptides into drug‐like molecules capable of engaging challenging targets. These building blocks enhance stability, permeability, and bioavailability, accelerating the development of next‐generation peptide therapeutics.
Krishna K. Sharma, Komal Sharma, Anku Sharma, Kamya Rao, Rahul Jain, Brett VanVeller   +5 more
wiley   +2 more sources

Amelioration of injury-induced tissue acidosis by a nonsteroidal analgesic attenuates antinociceptive effects of the pH-dependent opioid agonist NFEPP

Scientific Reports, 2022
Opioid agonists are powerful drugs for managing pain. However, their central side effects are limiting their use and drugs with similar potency, but a lower risk profile are needed. (±)-N-(3-fluoro-1-phenethylpiperidine-4-yl)-N-phenylpropionamide (NFEPP)
Melih Ö. Celik, Roger Negrete, Riccardo Di Rosso, Halina Machelska, Christoph Stein   +4 more
doaj   +1 more source

Benzodiazepine receptors and the control of ingestive behaviour in the rat [PDF]

, 1996
When administered systemically, benzodiazepine receptor agonists have been shown to increase food intake in a number of species. Conversely, benzodiazepine receptor inverse agonists bring about reliable decreases in feeding.
Higgs, Suzanne, Higgs, S
core  

qcGEM: A Graph‐Based Molecular Representation With Quantum Chemistry Awareness

Advanced Science, EarlyView.
In this work, we introduce qcGEM, a quantum‐chemistry‐aware graph‐based embedding of molecules that incorporates physical priors into molecular representation learning. Through a specially designed model architecture to adequately process quantum chemistry information as well as three‐dimensional molecular geometry, qcGEM provides a compact, physics ...
Haoyu Wang, Ziyan Zhang, Swee Hong Ng, Haipeng Gong   +3 more
wiley   +1 more source

Common Mechanisms Underlying Opioid Tolerance and Dependence and Neuropathic Pain: Role of Metabotropic Glutamate Receptors

Pain Research and Management, 2000
It has been suggested that opioid tolerance and dependence share common mechanisms with neuropathic pain. This short review deals with the role of glutamate and glutamate receptors in opioid tolerance and dependence, and neuropathic pain.
Marian E Fundytus
doaj   +1 more source

Opioid and GABAB receptors differentially couple to an adenylyl cyclase/protein kinase A downstream effector after chronic morphine treatment.

Frontiers in Pharmacology, 2014
Opioids are intensely addictive, and cessation of their chronic use is associated with a highly aversive withdrawal syndrome. A cellular hallmark of withdrawal is an opioid sensitive protein kinase A-dependent increase in GABA transporter-1 (GAT-1 ...
Elena Elizabeth Bagley
doaj   +1 more source

Buprenorphine-Induced Antinociception Is Mediated by μ-Opioid Receptors and Compromised by Concomitant Activation of Opioid Receptor-Like Receptors

, 2003
Buprenorphine is a mixed opioid receptor agonist-antagonist used clinically for maintenance therapy in opiate addicts and pain management. Dose-response curves for buprenorphine-induced antinociception display ceiling effects or are bell shaped, which ...
Takeshima, Hiroshi, Saliminejad, Nazli, Walwyn, Wendy, Shoshana Eitan, Eitan, Shoshana, Christopher J. Evans, Brigitte L. Kieffer, Bryant, Camron, Kieffer, Brigitte, Hiroshi Takeshima, Yang, Yu, Carroll, F. Ivy, Maidment, Nigel, Camron D. Bryant, Wendy Walwyn, F. Ivy Carroll, Yu C. Yang, Nazli Saliminejad, Evans, Christopher, Lutfy, Kabirullah, Nigel T. Maidment, Kabirullah Lutfy   +21 more
core   +1 more source

Social trauma and the mu-opioid system in depression [PDF]

, 2011
The overarching thesis under investigation is that the endogenous opioid system plays a key role in depression subsequent to traumatic childhood social experiences. This is suggested by the fact that animal work indicates that mu-opioids robustly mediate
Malcolm-Smith, Susan
core   +1 more source

Analgesia linked to Nav1.7 loss of function requires µ- and δ-opioid receptors [version 1; referees: 2 approved]

Wellcome Open Research, 2018
Background: Functional deletion of the Scn9a (sodium voltage-gated channel alpha subunit 9) gene encoding sodium channel Nav1.7 makes humans and mice pain-free. Opioid signalling contributes to this analgesic state.
Vanessa Pereira, Queensta Millet, Jose Aramburu, Cristina Lopez-Rodriguez, Claire Gaveriaux-Ruff, John N. Wood   +5 more
doaj   +1 more source