Results 11 to 20 of about 10,682 (172)

Quinazoline-2,4(1H,3H)-dione derivatives as new class of CB1 Agonists: A pharmacophore-based virtual screening workflow and drug discovery [version 3; peer review: 2 approved, 1 approved with reservations] [PDF]

F1000Research
Background The cannabinoid 1 (CB1) receptor is the primary target of Δ9-tetrahydrocannabinol (Δ9-THC), the psychoactive component of cannabis sativa (commonly known as “kif” in Morocco).
Fouad Khalil, Abdellah EL AISSOUQ, MOURAD STITOU, Mohamed Enneiymy, Said El Rhabori, Hicham Zaitan, Abdelkrim Ouammou   +6 more
doaj   +2 more sources

Crystal structures of agonist-bound human cannabinoid receptor CB1. [PDF]

Nature, 2017
The cannabinoid receptor 1 (CB1) is the principal target of the psychoactive constituent of marijuana, the partial agonist Δ9-tetrahydrocannabinol (Δ9-THC). Here we report two agonist-bound crystal structures of human CB1 in complex with a tetrahydrocannabinol (AM11542) and a hexahydrocannabinol (AM841) at 2.80 Å and 2.95 Å resolution, respectively ...
Tian, Hua, Kiran, Vemuri, Spyros P, Nikas, Robert B, Laprairie, Yiran, Wu, Lu, Qu, Mengchen, Pu, Anisha, Korde, Shan, Jiang, Jo-Hao, Ho, Gye Won, Han, Kang, Ding, Xuanxuan, Li, Haiguang, Liu, Michael A, Hanson, Suwen, Zhao, Laura M, Bohn, Alexandros, Makriyannis, Raymond C, Stevens, Zhi-Jie, Liu   +19 more
openaire   +4 more sources

Cannabinoid Modulation of Excitability and Short-Term Neuronal Dynamics in the Dorsal and Ventral Hippocampus [PDF]

Biology
Endocannabinoids, acting primarily through CB1 receptors, are critical modulators of neuronal activity, influencing cognitive functions and emotional processing.
Giota Tsotsokou, Ioanna-Maria Sotiropoulou, Klearchos Stampolitis, George D. Oikonomou, Aikaterini-Paraskevi Avdi, Costas Papatheodoropoulos   +5 more
doaj   +2 more sources

Development of a Heuristic Machine Analogy Method for Model Simplification With an Application to a Large‐Scale Model of Gi/Gs Signaling [PDF]

CPT: Pharmacometrics & Systems Pharmacology
Model simplification is a process to simplify large‐scale mathematical models to enable easy applications such as simulation and parameter estimation.
Liang Yang, David Finlay, Michelle Glass, Stephen Duffull   +3 more
doaj   +2 more sources

Cannabinoid CB1 receptor agonist ACEA alleviates brain ischemia/reperfusion injury via CB1–Drp1 pathway [PDF]

Cell Death Discovery, 2020
AbstractActivation of the cannabinoid CB1 receptor induces neuroprotection against brain ischemia/reperfusion injury (IRI); however, the mechanism is still unknown. In this study, we used oxygen-glucose deprivation/reoxygenation (OGD/R)-induced injury in neuronal cells and middle cerebral artery occlusion (MCAO)-induced brain IRI in rats to mimic ...
Yang, Shuai, Hu, Bin, Wang, Zongming, Zhang, Changming, Jiao, Haosen, Mao, Zhigang, Wei, Liguang, Jia, Ji, Zhao, Jingling   +8 more
openaire   +2 more sources

Cannabinoid Receptor 1 Agonist ACEA and Cannabinoid Receptor 2 Agonist GW833972A Attenuates Cell-Mediated Immunity by Different Biological Mechanisms

Cells, 2023
Cannabinoid receptor 1 (CB1) and cannabinoid receptor 2 (CB2) are components in the endocannabinoid system that play significant roles in regulating immune responses. There are many agonists for the cannabinoid receptors; however, their effects on T cell
Nuchjira Takheaw, Kanyaruck Jindaphun, Supansa Pata, Witida Laopajon, Watchara Kasinrerk   +4 more
doaj   +1 more source

Cannabinoid receptor 1 positive allosteric modulator (GAT229) attenuates cisplatin-induced neuropathic pain in mice

Saudi Pharmaceutical Journal, 2023
Chemotherapy-induced peripheral neuropathy (CIPN) is one of chemotherapies’ most often documented side effects. Patients with CIPN experience spontaneous burning, numbness, tingling, and neuropathic pain in their feet and hands.
Amina M. Bagher, Lenah S. Binmahfouz, Rasheed A. Shaik, Basma G. Eid   +3 more
doaj   +1 more source

Circuit-Selective FAAH Inhibition Suppresses Experimental Absence Seizures. [PDF]

CNS Neurosci Ther
Selective inhibition of FAAH with PF‐04457845 enhances endogenous AEA signaling and suppresses absence seizures in Genetic Absence Epilepsy Rats from Strasbourg (GAERS). Video‐EEG recordings demonstrate a marked reduction in SWDs following both acute and subchronic FAAH inhibitions.
Morais TP, Bombardi C, Crunelli V, Di Giovanni G.   +3 more
europepmc   +2 more sources

Improved cyclobutyl nabilone analogs as potent CB1 receptor agonists

European Journal of Medicinal Chemistry, 2022
In earlier work, we explored the SAR for the C3 side chain pharmacophore in the hexahydrocannabinol template represented by the drug nabilone, which resulted in the development of AM2389. In an effort for further optimization, we have merged features of nabilone and AM2389 and explored the C3 side chain with varying chain lengths and terminal ...
Ioannis P. Papanastasiou, Markos-Orestis Georgiadis, Christos Iliopoulos-Tsoutsouvas, Carol A. Paronis, Christina A. Brust, Ngan K. Tran, Lipin Ji, Xiaoyu Ma, JodiAnne T. Wood, Nikolai Zvonok, Fei Tong, Laura M. Bohn, Spyros P. Nikas, Alexandros Makriyannis   +13 more
openaire   +3 more sources

CB1 Cannabinoid Receptor Signaling and Biased Signaling

Molecules, 2021
The CB1 cannabinoid receptor is a G-protein coupled receptor highly expressed throughout the central nervous system that is a promising target for the treatment of various disorders, including anxiety, pain, and neurodegeneration.
Luciana M. Leo, Mary E. Abood
doaj   +1 more source