Results 71 to 80 of about 2,269 (179)

Cannabinoid CB2 receptor‐mediated analgesia: mechanism‐based insights and therapeutic potential

British Journal of Pharmacology, Volume 182, Issue 21, Page 5090-5118, November 2025.
Agonists of the cannabinoid 2 (CB2) receptor have shown promise for the treatment of pain in a variety of animal models. However, despite current preclinical evidence supporting the use of CB2 agonists for pain, successful translation of findings from preclinical models to human patients is lacking.
Kelsey G. Guenther, Andrea G. Hohmann
wiley   +1 more source

Melanocortins and agouti-related protein modulate the excitability of two arcuate nucleus neuron populations by alteration of resting potassium conductances [PDF]

, 2006
The hypothalamic melanocortin system is crucial for the control of appetite and body weight. Two of the five melanocortin receptors, MC3R and MC4R are involved in hypothalamic control of energy homeostasis, with the MC4R having the major influence. It is
Acuna-Goycolea, Balthasar, Bays, Bednarek, Bonilla, Burdakov, Butler, Choudhury, Cone, Cowley, Cowley, Dhillon, Erickson, Fan, Farooqi, Fekete, Graham, Gropp, Hagan, Harrold, Haskell-Luevano, Hille, Huszar, Ibrahim, Kanjhan, Kas, Kim, Kim, Lechan, Liu, Liu, Mountjoy, Nijenhuis, Plum, Ramos, Roseberry, Srinivasan, Takano, Tang, Wang, Wikberg, Yang   +41 more
core   +4 more sources

Atrium-Specific Kir3.x Determines Inducibility, Dynamics, and Termination of Fibrillation by Regulating Restitution-Driven Alternans [PDF]

Circulation, 2013
Background— Atrial fibrillation is the most common cardiac arrhythmia. Ventricular proarrhythmia hinders pharmacological atrial fibrillation treatment. Modulation of atrium-specific Kir3.x channels, which generate a constitutively active current ( I K,ACh-c ) after atrial
Bingen, B.O., Neshati, Z., Askar, S.F.A., Kazbanov, I.V., Ypey, D.L., Panfilov, A.V., Schalij, M.J., Vries, A.A.F. de, Pijnappels, D.A.   +8 more
openaire   +3 more sources

Discovery, characterization and structure-activity relationships of an inhibitor of inward rectifier potassium (Kir) channels with preference for Kir2.3, Kir3.X and Kir7.1

Frontiers in Pharmacology, 2011
The inward rectifier family of potassium (Kir) channels is comprised of at least 16 family members exhibiting broad and often overlapping cellular, tissue or organ distributions.
Jerod S Denton
doaj   +1 more source

Mass spectrometric analysis reveals a functionally important PKA phosphorylation site in a Kir3 channel subunit [PDF]

Pflügers Archiv - European Journal of Physiology, 2009
Phosphorylation of the Kir3 channel by cAMP-dependent protein kinase (PKA) potentiates activity and strengthens channel-PIP(2) interactions, whereas phosphorylation by protein kinase C (PKC) exerts the opposite effects (Keselman et al., Channels 1:113-123, 2007; Lopes et al., Channels 1:124-134, 2007).
Radda, Rusinova, Yu-Ming Albert, Shen, Georgia, Dolios, Julio, Padovan, Heyi, Yang, Madeleine, Kirchberger, Rong, Wang, Diomedes E, Logothetis   +7 more
openaire   +2 more sources

Progress on the development of Class A GPCR‐biased ligands

British Journal of Pharmacology, Volume 182, Issue 14, Page 3249-3300, July 2025.
Class A G protein‐coupled receptors (GPCRs) continue to garner interest for their essential roles in cell signalling and their importance as drug targets. Although numerous drugs in the clinic target these receptors, over 60% GPCRs remain unexploited. Moreover, the adverse effects triggered by the available unbiased GPCR modulators, limit their use and
Paula Morales, Magdalena M. Scharf, Marcel Bermudez, Attila Egyed, Rafael Franco, Olivia K. Hansen, Nadine Jagerovic, Jan Jakubík, György M. Keserű, Dóra Judit Kiss, Pawel Kozielewicz, Olav Larsen, Maria Majellaro, Ana Mallo‐Abreu, Gemma Navarro, Rubén Prieto‐Díaz, Mette M. Rosenkilde, Eddy Sotelo, Holger Stark, Tobias Werner, Laura M. Wingler   +20 more
wiley   +1 more source

The Na+-Activated Potassium Channel Slack Shares a Similar Na+ Coordination Site with Kir3 Channels [PDF]

Biophysical Journal, 2010
Characteristics of Na+ activated potassium channel (Slack or Slo2.2) currents, including high conductance, rundown, regulation by Na+, Cl- and phosphorylation have long been reported but underlying mechanisms remain unknown. Here we report identification of a sodium regulatory site in the RCK2 domain of Slack channels by screening the C-terminus with ...
Zhang, Zhe, Rosenhouse-Dantsker, Avia, Tang, Qiongyao, Noskov, Sergei, Logothetis, Diomedes E.   +4 more
openaire   +1 more source

GABAB Receptor: Structure, Biological Functions, and Therapy for Diseases

MedComm, Volume 6, Issue 5, May 2025.
Within the GABAergic system, GABABRs are potential therapeutic targets for dealing multiple metabolic and binge eating disorders and food addiction. Allosteric modulators and small peptides targeting GABABR signaling pathways may be developed as attractive drug candidates that avoid the side effects of agents that directly bind these receptors ...
Weijie Xie, Yuan Li, Xinyue Wang, Elena Blokhina, Evgeny Krupitsky, Marina Vetrova, Ji Hu, Ti‐Fei Yuan, Jue Chen, Hua Wang, Xiangfang Chen   +10 more
wiley   +1 more source

Dronedarone. [PDF]

, 2009
Amiodarone is the most effective antiarrhythmic drug for maintaining sinus rhythm for patients with atrial fibrillation. Extra-cardiac side effects have been a limiting factor, especially during chronic use, and may offset its benefits.
Kowey, Peter R, Patel, Chinmay, Yan, Gan-Xin   +2 more
core   +1 more source

Ethosuximide: Subunit‐ and Gβγ‐dependent blocker and reporter of allosteric changes in GIRK channels

British Journal of Pharmacology, Volume 182, Issue 8, Page 1704-1718, April 2025.
Background and Purpose The antiepileptic drug ethosuximide (ETX) suppresses epileptiform activity in a mouse model of GNB1 syndrome, caused by mutations in Gβ1 protein, likely through the inhibition of G‐protein gated K+ (GIRK) channels. Here, we investigated the mechanism of ETX inhibition (block) of different GIRKs.
Boris Shalomov, Theres Friesacher, Daniel Yakubovich, J. Carlo Combista, Haritha P. Reddy, Shoham Dabbah, Harald Bernsteiner, Eva‐Maria Zangerl‐Plessl, Anna Stary‐Weinzinger, Nathan Dascal   +9 more
wiley   +1 more source