Results 171 to 180 of about 61,838 (257)

The chemokine receptor‐like fourth extracellular loop of the apelin receptor differentially regulates apelin and elabela binding and signalling

open access: yesBritish Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Apelin and Elabela are endogenous ligands of the apelin receptor (apelin receptor/APJ), a GPCR involved in cardiovascular regulation and body fluid homeostasis. The human receptor contains a conserved disulfide bridge linking the N‐terminal domain to extracellular loop 3 (ECL3) via Cys19 and Cys281, forming a structural ...
Chloé Bonef   +11 more
wiley   +1 more source

Muscarinic agonists for schizophrenia: Bridging preclinical evidence and clinical enthusiasm

open access: yesBritish Journal of Pharmacology, EarlyView.
Abstract Antipsychotic drugs targeting dopamine receptors have been used to treat schizophrenia for decades, primarily alleviating positive symptoms such as hallucinations and delusions. However, they provide limited benefit for cognitive and negative symptoms—major contributors to poor outcomes—and are frequently associated with significant side ...
Brian J. Morris, Judith A. Pratt
wiley   +1 more source

Comprehensive in vitro profiling of traditional and emerging stimulants at monoamine transporters and the 5‐HT2A receptor

open access: yesBritish Journal of Pharmacology, EarlyView.
A pharmacological profiling of 58 synthetic stimulants of various classes at dopamine, norepinephrine, and serotonin transporters and the 5‐HT2A receptor, most showing distinct class‐dependent profiles, with some indicating a high abuse potential. Background and Purpose New psychoactive substances (NPSs) often emerge on the illicit drug market with ...
Darta Stalberga   +9 more
wiley   +1 more source

Potentiation effects of the positive allosteric modulator PTC‐174 on NMDA receptors in neonatal male rat substantia nigra dopaminergic neurons

open access: yesBritish Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Positive allosteric modulators bind to secondary binding sites on the receptor and alter receptor conformation and activation, changing agonist potency and efficacy. PTC‐174 is a novel NMDA receptor positive allosteric modulator that particularly enhances activity of receptors containing GluN2C or GluN2D subunits.
Bangyuan Liu, Alasdair J. Gibb
wiley   +1 more source

Novel Histopathologic Features of Diffuse Blue‐Gray Hyperpigmentation Associated With Kratom Use: A Case Report and Literature Review

open access: yesJournal of Cutaneous Pathology, EarlyView.
ABSTRACT Background Drug‐induced hyperpigmentation accounts for 10%–20% of acquired pigmentary disorders and can be misdiagnosed for other causes such as melasma, post inflammatory changes, or heavy metal deposition. Kratom (Mitragyna speciosa), a Southeast Asian plant with an opioid‐like profile, has been increasingly used in the United States for ...
Rita Kamoua   +4 more
wiley   +1 more source

Amylin: A Multi‐Functional Pancreatic Hormone—A Review

open access: yesDiabetes, Obesity and Metabolism, EarlyView.
ABSTRACT Amylin is a pancreatic beta‐cell hormone that sits at a systems hub connecting key aspects of energy metabolism. Amylin physiologically controls satiation, slows gastric emptying and limits postprandial glucagon release, while its actions also link homeostatic eating controls with reward driven behaviours via defined central nervous system ...
Christelle Le Foll, Thomas A. Lutz
wiley   +1 more source

Efficacy and target engagement of dopamine agonist pramipexole for anhedonic depression - the PRIME-PRAXOL randomized controlled trial

open access: yes
Ventorp F   +20 more
europepmc   +1 more source

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