Concentration-response curves (CRCs) are characterized by a midpoint (EC50) and high-concentration asymptote (POmax) that relate to the agonist's affinity efficacy. Recently, third agonist attribute, efficiency, was defined as fraction of ligand binding energy is applied conformational change activates receptor. We show efficiency can be calculated from EC50 POmax estimate its value for 17 agon...

Abstract: Background/Aim: Alzheimer’s disease (AD), a type of neurodegenerative disorder, possesses significant memory loss as one the cardinal manifestations. The pathophysiology AD includes increased accumulation A?, degeneration cholinergic activity and mitochondrial dysfunction. Nicotinic acetylcholine receptors (nAChRs) especially alpha7 nicotinic (?7 nAChRs) are widely distributed in brai...

Acetylcholine (ACh), acting via muscarinic receptors, is known to modulate neuronal responsiveness in primary sensory neocortex. The administration of ACh to cortical neurons facilitates or suppresses responses to sensory stimuli, and these effects can endure well beyond the period of ACh application. In the present study, we sought to determine whether ACh produces a general change in sensory ...

The first model of G-protein-K(ACh) channel interaction was developed 14 years ago and then expanded to include both the receptor-G-protein cycle and G-protein-K(ACh) channel interaction. The G-protein-K(ACh) channel interaction used the Monod-Wyman-Changeux allosteric model with the idea that one K(ACh) channel is composed of four subunits, each of which binds one active G-protein subunit (G(b...

Muscarinic autoreceptors modulate cholinergic neurotransmission in animals ranging from insects to humans. No previous studies have characterized autoreceptor modulation of acetylcholine (ACh) release in prefrontal cortex of intact mouse. Data obtained from experiments in 45 mice considered ACh as a phenotype and tested the hypothesis that pharmacologically defined M2 receptors modulate ACh rel...

Nicotine alters the developmental trajectory of acetylcholine (ACh) systems in the immature brain, with vulnerability extending from fetal stages through adolescence. We administered nicotine to adolescent rats (postnatal days PN30-47) and then examined the subsequent response to nicotine given in adulthood (PN90-107), simulating plasma levels in smokers, and performing evaluations during nicot...

Diverse nicotinic acetylcholine receptor (nAChR) subtypes containing different subunit combinations can be placed on nerve terminals or soma/dendrites in the ventral tegmental area (VTA). nAChR α6 subunit message is abundant in the VTA, but α6*-nAChR cellular localization, function, pharmacology, and roles in cholinergic modulation of dopaminergic (DA) neurons within the VTA are not well unders...

BACKGROUND Developmental exposure to a wide variety of developmental neurotoxicants, including organophosphate pesticides, evokes late-emerging and persistent abnormalities in acetylcholine (ACh) systems. We are seeking interventions that can ameliorate or reverse the effects later in life. OBJECTIVES We administered parathion to neonatal rats and then evaluated whether a high-fat diet begun ...

In the present study, we explored the effect of acetylcholine (ACh) on lymphocyte function and the receptor mechanisms mediating the effect. Concanavalin A (Con A)-induced interleukin-2 (IL-2) production and natural killer (NK) cell cytotoxicity were used to assess function of the T lymphocytes and the NK cells from rat spleens. Muscarinic ACh receptors (mA ChRs) agonist pilocarpine and antagon...

Acetylcholine (ACh) has a crucial role in the peripheral and central nervous systems. The enzyme choline acetyltransferase (ChAT) is responsible for synthesizing ACh from acetyl-CoA and choline in the cytoplasm and the vesicular acetylcholine transporter (VAChT) uptakes the neurotransmitter into synaptic vesicles. Following depolarization, ACh undergoes exocytosis reaching the synaptic cleft, w...