A5018667385- Neuroscience and Neuropharmacology Research
- Receptor Mechanisms and Signaling
- Neuropeptides and Animal Physiology
- Cholinesterase and Neurodegenerative Diseases
- Circadian rhythm and melatonin
- Neurotransmitter Receptor Influence on Behavior
- Melanoma and MAPK Pathways
- Pharmacological Receptor Mechanisms and Effects
- Hypothalamic control of reproductive hormones
- Molecular Sensors and Ion Detection
- Phenothiazines and Benzothiazines Synthesis and Activities
- Neuroinflammation and Neurodegeneration Mechanisms
- Alzheimer's disease research and treatments
- Pain Mechanisms and Treatments
- Sleep and Wakefulness Research
- Ion channel regulation and function
- Sleep and related disorders
- Protein Kinase Regulation and GTPase Signaling
- Endoplasmic Reticulum Stress and Disease
- Ubiquitin and proteasome pathways
- Nicotinic Acetylcholine Receptors Study
- RNA regulation and disease
- Protein Tyrosine Phosphatases
- Cardiac electrophysiology and arrhythmias
- Bone and Dental Protein Studies
Aptuit (Italy)
2017-2022
GlaxoSmithKline (Italy)
2003-2013
Discovery Centre
2010
GlaxoSmithKline (United Kingdom)
2006
Substance P exerts its various biochemical effects mainly via interactions through neurokinin-1 receptors (NK1). Recently, the NK1 receptor has attracted considerable interest for possible role in a variety of psychiatric disorders including depression and anxiety. However, little is known regarding anatomical distribution human central nervous system (CNS). Riboprobe situ hybridization, quantitative PCR vitro autoradiography were performed. Highest mRNA levels localized locus coeruleus...
A pharmacophore model for triple reuptake inhibitors and the new class of 1-(aryl)-6-[alkoxyalkyl]-3-azabicyclo[3.1.0]hexanes were recently reported. Further investigation in this area led to identification a series potent selective endowed with good developability characteristics. Excellent bioavailability brain penetration are associated 6-(3,4-dichlorophenyl)-1-[(methyloxy)methyl]-3-azabicyclo[4.1.0]heptanes together high vitro potency selectivity at SERT, NET, DAT. In vivo microdialysis...
Abstract Introduction The neuronal mechanism driving Alzheimer's disease (AD) is incompletely understood. Methods Immunohistochemistry, pharmacology, biochemistry, and behavioral testing are employed in two pathological contexts—AD a transgenic mouse model—to investigate T14, 14mer peptide, as key signaling molecule the neuropathology. Results T14 increases AD brains progresses conspicuous 5XFAD mice, where its immunoreactivity corresponds to that seen AD: neurons immunoreactive for...
1 In this study, [(3)H]GR205171 (3(S)-(2-methoxy-5-(5-trifluoromethyltetrazol-1-yl)-phenylmethylamino)-2(S)-phenylpiperidine), a potent and selective NK1 receptor antagonist, was characterised in autoradiographic studies gerbil brain binding experiments on homogenates from human cortex striatum. 2 brain, highest levels of sites were observed caudate putamen, nucleus accumbens, medial cortical nuclei the amygdala intermediate detected hypothalamus, basolateral amygdala, septum, cortex. 3...
Histamine H(1) and serotonin 5-HT(2A) receptors mediate two different mechanisms involved in sleep regulation: antagonists are inducers, while maintainers. Starting from 9'a, a novel spirotetracyclic compound endowed with good H(1)/5-HT(2A) potency but poor selectivity, very high Cli, P450 profile, specific optimization strategy was set up. In particular, we investigated the possibility of introducing appropriate amino acid moieties to optimize developability profile series. Following this...
Abstract Increasing evidence suggests that substance P (SP) neurokinin‐1 (NK1) receptors are involved in stress and emotional responses, representing a potential target for the treatment of anxiety depression humans. Given important role amygdaloid complex regulation behavior, we examined mRNA levels preprotachykinin A [PPT‐A, precursor both SP neurokinin (NKA)] 3 H‐SP binding sites amygdala patients affected by bipolar disorder, major or schizophrenia as compared with matched control...