Single Inhaler LABA/LAMA for COPD
Chronic obstructive pulmonary disease (COPD) is a common disabling disease characterized by progressive airflow obstruction. Great efforts were spent in the development of drugs able to improve symptoms, quality of life, reduce exacerbations ...
Mario Malerba+10 more
doaj +1 more source
Presynaptic M1 muscarinic cholinoceptors mediate inhibition of excitatory synaptic transmission in the hippocampus in vitro [PDF]
The effects of the cholinoceptor agonist, carbachol (CCh), were examined in the rat hippocampal slice preparation. Intracellular recordings from CA1 pyramidal neurones revealed that CCh (1–3 μM) inhibited excitatory postsynaptic responses evoked by ...
Sheridan, Robert D., Sutor, Bernd
core +1 more source
Isosterism and Bioisosterism Case Studies with Muscarinic Agonists
The synthesis and activity of enantiomerically pure analogues of pilocarpine and muscarinic agonists with the azabicyclo[2.2.1]heptane skeleton is described.
Philipp Floersheim+2 more
doaj +2 more sources
Psychosis that occurs over the course of Alzheimer’s disease (AD) is associated with increased caregiver burden and a more rapid cognitive and functional decline.
Heidy Jimenez+9 more
doaj +1 more source
Deciphering the skeletal interoceptive circuitry to control bone homeostasis
This review introduces the skeletal interoceptive circuitry, covering the ascending signals from bone tissues to the brain (sensors), the central neural circuits that integrate this information and dispatch commands (CPU), and the descending pathways that regulate bone homeostasis (effectors).
Yefeng Wu+7 more
wiley +1 more source
Current and Future Issues in the Development of Spinal Agents for the Management of Pain. [PDF]
Targeting analgesic drugs for spinal delivery reflects the fact that while the conscious experience of pain is mediated supraspinally, input initiated by high intensity stimuli, tissue injury and/or nerve injury is encoded at the level of the spinal ...
Fisher, Casey J+3 more
core +2 more sources
Muscarinic and Nicotinic Contribution to Contrast Sensitivity of Macaque Area V1 Neurons
Acetylcholine is a neuromodulator that shapes information processing in different cortical and subcortical areas. Cell type and location specific cholinergic receptor distributions suggest that acetylcholine in macaque striate cortex should boost feed ...
Jose L. Herrero+2 more
doaj +1 more source
We have described the synthesis of a new series of LCAPs (long‐chain arylpiperazine) as serotoninergic ligands (FG 1‐18). The combination of structural elements including heterocyclic nucleus, propyl chain and 4,5‐dihydrothiazol‐2‐ylphenylpiperazines, led to the preparation of different derivatives tested for their affinity toward 5‐HT1A, 5‐HT2A and 5 ...
Giorgia Andreozzi+18 more
wiley +1 more source
Ligand regulation of the quaternary organization of cell surface M3 muscarinic acetylcholine receptors analyzed by fluorescence resonance energy transfer (FRET) imaging and homogenous time-resolved FRET [PDF]
Flp-In T-REx 293 cells expressing a wild type human M muscarinic acetylcholine receptor construct constitutively and able to express a Receptor Activated Solely by Synthetic Ligand (RASSL) form of this receptor on demand maintained response to the ...
Alvarez-Curto, Elisa+3 more
core +2 more sources
Open and Closed Triple Inhaler Therapy in Patients with Uncontrolled Asthma
Long-acting muscarinic antagonists (LAMAs) are a class of inhalers that has recently been included as add-on therapy in the GINA guidelines, either in a single inhaler device with inhaled corticosteroids plus long-acting β2-agonists (ICS + LABA) (closed ...
Serafeim-Chrysovalantis Kotoulas+5 more
doaj +1 more source