Results 81 to 90 of about 28,193 (228)

Preclinical models for evaluating psychedelics in the treatment of major depressive disorder

British Journal of Pharmacology, EarlyView.
Psychedelic drugs have seen a resurgence in interest as a next generation of psychiatric medicines with potential as rapid‐acting antidepressants (RAADs). Despite promising early clinical trials, the mechanisms which underlie the effects of psychedelics are poorly understood.
Laith Alexander, Dasha Anderson, Luke Baxter, Matthew Claydon, James Rucker, Emma S. J. Robinson   +5 more
wiley   +1 more source

PDE4D and PDE3B orchestrate distinct cAMP microdomains in 3T3‐L1 adipocytes

British Journal of Pharmacology, EarlyView.
Basal conditions: •Ins/PDE3B lowers cytoplasmic cAMP (cyt‐cAMP) without affecting plasma membrane cAMP (pm‐cAMP). •Insulin decreases lipid droplet cAMP (LD‐cAMP) independent of PDE3B. •FGF1/PDE4D modestly reduces both cyt‐ and pm‐cAMP, while PDE4D alone can modulate LD‐cAMP. ISO stimulation: •Ins/PDE3B has minimal impact on cyt‐cAMP.
Johannes Krier, David Spähn, David Arturo Juarez Lopez, Judith L. Nono, Judith Seigner, Lisa Jacob, Siegfried Ussar, Robert Lukowski, Andreas L. Birkenfeld, Gencer Sancar   +9 more
wiley   +1 more source

Consequences of cystic fibrosis transmembrane regulator mutations on inflammatory cells [PDF]

, 2016
Recent studies in cystic fibrosis (CF) transmembrane regulator (CFTR) mutations and function have shed light on its involvement in disease progression. The extent of cell and tissue distribution of CFTR facilitates systemic dysfunction of ion transport ...
Castro, Guillermo Raul, Grumelli, Sandra, Islan, German Abel   +2 more
core   +1 more source

Novel approaches for drug development against chronic primary pain: A systematic review

British Journal of Pharmacology, EarlyView.
Abstract Chronic primary pain (CPP) persisting for more than 3 months, associated with significant emotional distress without any known underlying cause, is an unmet medical need. Traditional or adjuvant analgesics do not provide satisfactory pain relief for a great proportion of these patients.
Valéria Tékus, Éva Borbély, Andreas Goebel, Ralf Baron, Zsófia Hajna, Zsuzsanna Helyes   +5 more
wiley   +1 more source

Nanodelivery of a functional membrane receptor to manipulate cellular phenotype. [PDF]

, 2018
Modification of membrane receptor makeup is one of the most efficient ways to control input-output signals but is usually achieved by expressing DNA or RNA-encoded proteins or by using other genome-editing methods, which can be technically challenging ...
Baikoghli, Mo, Cheng, R Holland, Coleman, Matthew A, He, Wei, Patriarchi, Tommaso, Shen, Ao, Tian, Lin, Xiang, Yang K   +7 more
core   +2 more sources

Cancer pain: current practice and emerging targets

British Journal of Pharmacology, EarlyView.
Cancer pain (CP) arises from a complex interplay between the tumour and its microenvironment. Many patients experience a mixed pain phenotype that encompasses nociceptive, neuropathic and neuroinflammatory mechanisms, and vary across tumour type and disease stage. Despite decades of intensive research, the mainstay of cancer pain treatment is still non‐
Yi Ye, Marcin Chwistek, Zhiting Gong, Vanessa Uzonwanne, Xiaojie Shi, Arpad Szallasi   +5 more
wiley   +1 more source

Inflammation produces catecholamine resistance in obesity via activation of PDE3B by the protein kinases IKKε and TBK1. [PDF]

, 2013
Obesity produces a chronic inflammatory state involving the NFκB pathway, resulting in persistent elevation of the noncanonical IκB kinases IKKε and TBK1.
Chang, Louise, Chiang, Shian-Huey, Leto, Dara, Mowers, Jonathan, Reilly, Shannon M, Saltiel, Alan R, Simon, Joshua, Uhm, Maeran   +7 more
core   +3 more sources

The substance P receptor, which couples to Gq/11, is a substrate of beta-adrenergic receptor kinase 1 and 2

Journal of Biological Chemistry, 1993
The agonist-occupied forms of several G-protein-coupled receptors that modulate the activity of adenylycyclase via Gs (e.g. beta 2-adrenergic) or Gi (e.g. alpha 2-adrenergic and cardiac muscarinic) are phosphorylated by beta-adrenergic receptor kinases (beta ARK 1 and beta ARK 2).
M M, Kwatra, D A, Schwinn, J, Schreurs, J L, Blank, C M, Kim, J L, Benovic, J E, Krause, M G, Caron, R J, Lefkowitz   +8 more
openaire   +2 more sources

Therapeutic potential of small molecules that block receptor‐induced Kv7/M‐current suppression in neuroprotection, seizures, and pain

British Journal of Pharmacology, EarlyView.
Receptor‐induced Kv7/M‐current suppression increases neuronal activity and contributes to pathology of several conditions. A new class of Kv7 modulators identified in this study attenuates M‐current suppression and shows therapeutic effects. Abstract Background and Purpose Neuronal Kv7 channels generate low voltage–gated potassium currents known as the
Young Woo Kim, Pavan Kumar Behara, Lamees Alhassen, Cindy Wong, Olivier Civelli, Naoto Hoshi   +5 more
wiley   +1 more source

Glycogen synthase kinases 3α and 3β in cardiac myocytes: regulation and consequences of their inhibition [PDF]

, 2008
Inhibition of glycogen synthase kinase 3β (GSK3β) as a consequence of its phosphorylation by protein kinase B/Akt (PKB/Akt) has been implicated in cardiac myocyte hypertrophy in response to endothelin-1 or phenylephrine.
Alsafi, Ali, Clerk, Angela, Cullingford, Timothy E., Fuller, Stephen John, Giraldo Ramirez, Alejandro, Markou, Thomais, Sugden, Peter H., Weiss, Sophie C.   +7 more
core   +1 more source