Synthesis and Evaluation of Fluorinated Peptidomimetics Enabling the Development of <sup>18</sup>F-Labeled Radioligands Targeting Muscarinic Acetylcholine Receptor Subtype M3. [PDF]
Fluorinated peptidomimetics targeting muscarinic acetylcholine receptor subtype M3: Fluorinated peptidomimetic compounds based on a β‐alanine‐glycine scaffold, with lead compound 24 demonstrating high M3 selectivity and submicromolar potency. The first M3‐selective positron emission tomography radioligand, [18F]24, is synthesized and will be evaluated ...
Herrera-Rueda MA +4 more
europepmc +2 more sources
A molecular basis for selective antagonist destabilization of dopamine D3 receptor quaternary organization [PDF]
The dopamine D3 receptor (D3R) is a molecular target for both first-generation and several recently-developed antipsychotic agents. Following stable expression of this mEGFP-tagged receptor, Spatial Intensity Distribution Analysis indicated that a ...
Caltabiano, Gianluigi +6 more
core +2 more sources
The dopamine transporter (DAT) clears neurotransmitters from the extracellular space and serves as an important regulator of signal amplitude and duration at sites of dopamine release. Several different intracellular signaling pathways have been observed
Suzanne M. Underhill, Susan G. Amara
doaj +1 more source
Relationship between membrane phosphatidylinositol-4,5-bisphosphate and receptor-mediated inhibition of native neuronal M channels [PDF]
The relationship between receptor-induced membrane phosphatidylinositol-4'5'-bisphosphate (PIP2) hydrolysis and M-current inhibition was assessed in single-dissociated rat sympathetic neurons by simultaneous or parallel recording of membrane current and ...
Abogadie, FC +6 more
core +1 more source
In the prefrontal cortex, dopamine D1-like and M1 muscarinic receptors are both involved in the regulation of attentional, cognitive and emotional processes but so far no information has been provided on their functional interaction. In the present study
Maria C. Olianas +2 more
doaj +1 more source
The constitutive secretion of antioxidant Cu-Zn Superoxide dismutase (SOD1) has been widely demonstrated in many cellular lines. In addition, we showed that as well as the basal SOD1 secretion, this enzyme is also exported through depolarization of ...
Simona Damiano +8 more
doaj +1 more source
Changes in adrenergic and cholinergic receptors on human cerebral vessels. Implications for new therapeutic strategies in Alzheimer's Disease [PDF]
Abstract Background Sporadic cerebral amyloid angiopathy (CAA) occurs as a result of a failure of Intramural Periarterial Drainage (IPAD) of amyloid‐beta (Aβ) along the walls of capillaries and arteries. The motive force for IPAD is provided by the spontaneous contractions of cerebrovascular smooth muscle cells (CVSMC that receive adrenergic and ...
Carare R.
europepmc +2 more sources
Purification and properties of m1-toxin, a specific antagonist of m1 muscarinic receptors [PDF]
The venom of the Eastern green mamba from Africa, Dendroaspis angusticeps, was found to block the binding of 3H-quinuclidinyl benzilate to pure m1 and m4 muscarinic ACh receptors expressed in Chinese hamster ovary cells. The principal toxin in the venom with anti- m1 muscarinic activity was purified by gel filtration and reversed- phase HPLC.
S I, Max, J S, Liang, L T, Potter
openaire +2 more sources
Thrombin Protease-activated Receptor-1 Signals through Gq- and G13-initiated MAPK Cascades Regulating c-Jun Expression to Induce Cell Transformation [PDF]
Although the ability of G protein-coupled receptors to stimulate normal and aberrant cell growth has been intensely investigated, the precise nature of the molecular mechanisms underlying their transforming potential are still not fully understood.
Gutkind, J. Silvio +4 more
core +1 more source
Status epilepticus: Updates on mechanisms and treatments
Abstract Status epilepticus (SE) consists of prolonged, self‐sustaining seizures and is a common neurological emergency that causes respiratory compromise and neuronal injury. Without prompt treatment, the seizures can become resistant to benzodiazepines, leading to the progressive evolution of established, refractory, and super‐refractory SE.
Suchitra Joshi, Jaideep Kapur
wiley +1 more source

