A5076880355- Receptor Mechanisms and Signaling
- Neurotransmitter Receptor Influence on Behavior
- Neuroscience and Neuropharmacology Research
- Neuropeptides and Animal Physiology
- Pharmacological Receptor Mechanisms and Effects
- Computational Drug Discovery Methods
- Ion channel regulation and function
- Protein Kinase Regulation and GTPase Signaling
- Neuroendocrine regulation and behavior
- Pharmacological Effects and Assays
- Nitric Oxide and Endothelin Effects
- Treatment of Major Depression
- Cancer, Stress, Anesthesia, and Immune Response
- Cellular transport and secretion
- Ion Transport and Channel Regulation
- Neurological disorders and treatments
- Phosphodiesterase function and regulation
- Adenosine and Purinergic Signaling
- Monoclonal and Polyclonal Antibodies Research
- Pancreatic function and diabetes
- Stress Responses and Cortisol
- Microbial Community Ecology and Physiology
- Hormonal Regulation and Hypertension
- Renin-Angiotensin System Studies
- Enterobacteriaceae and Cronobacter Research
National Institutes of Health
2015-2024
National Institute of Neurological Disorders and Stroke
2015-2024
National Institute on Drug Abuse
2019-2021
McGill University Health Centre
2021
Chimerix (United States)
2021
University of Nottingham
2021
University of Leeds
2019
Monash University
1996-2018
National Center for Advancing Translational Sciences
2014-2018
University of North Carolina at Chapel Hill
2018
The striatum, which is the major component of basal ganglia in brain, regulated part by dopaminergic input from substantia nigra. Severe movement disorders result loss striatal dopamine patients with Parkinson's disease. Rats lesions nigrostriatal pathway caused 6-hydroxydopamine (6-OHDA) serve as a model for disease and show alterations gene expression two output systems striatum to globus pallidus Striatopallidal neurons 6-OHDA-induced elevation their specific messenger RNAs (mRNAs)...
We have used the polymerase chain reaction technique to selectively amplify a guanine nucleotide-binding protein-coupled receptor cDNA sequence from rat striatal mRNA that exhibits high homology previously cloned serotonin receptors. Sequencing of full length clone isolated library revealed an open reading frame 1311 base pairs, encoding 437-residue protein with seven hydrophobic regions. Within these regions, this was found be 41-36% identical following [5-hydroxytryptamine (5-HT)]...
We have utilized the polymerase chain reaction technique to selectively amplify a G protein-coupled receptor cDNA from rat kidney proximal convoluted tubule mRNA, which exhibits high homology with previously cloned serotonin receptors. Sequencing of full-length clone isolated hippocampal library revealed an open reading frame 1,212 base pairs encoding 404-residue protein seven hydrophobic regions predicted represent transmembrane-spanning domains. Within transmembrane regions, this was found...
While most effects of dopamine in the brain are mediated by D1 and D2 receptor subtypes, other members this G protein-coupled family have potentially important functions. D3 receptors belong to D2-like subclass receptors, activation which inhibits adenylyl cyclase. Using targeted mutagenesis mouse embryonic stem cells, we generated mice lacking functional receptors. A premature chain-termination mutation was introduced gene after residue Arg-148 second intracellular loop predicted protein...
In order to clone the D1 dopamine receptor linked adenylyl cyclase activation, polymerase chain reaction was used with highly degenerate primers selectively amplify a cDNA sequence from NS20Y neuroblastoma cell mRNA. This amplification produced fragment exhibiting considerable homology guanine nucleotide-binding (G)-protein-coupled receptors that have been cloned previously. To characterize this further, full-length isolated rat striatal library by using as probe. Sequence analysis of...
Abstract Designer Receptors Exclusively Activated by Drugs (DREADDs) are a popular chemogenetic technology for manipulation of neuronal activity in uninstrumented awake animals with potential human applications as well. The prototypical DREADD agonist clozapine N- oxide (CNO) lacks brain entry and converts to clozapine, making it difficult apply basic translational applications. Here we report the development two novel agonists, JHU37152 JHU37160, first dedicated 18 F positron emission...
We describe the cloning and characterization of a human 5-HT6 serotonin receptor. The open reading frame is interrupted by two introns in positions corresponding to third cytoplasmic loop extracellular loop. cDNA encodes 440-amino-acid polypeptide whose sequence diverges significantly from that published for rat Resequencing revealed sequencing error producing shift within frame. amino acid 89% similar corrected sequence. recombinant receptor positively coupled adenylyl cyclase has...
The interactions of dopaminergic agonists and antagonists with binding sites in bovine anterior pituitary membranes have been investigated radioligand-binding techniques computer-modeling procedures. 3H-labeled agonist is stereospecific, reversible, saturable, high affinity. rank order catecholamines, phenothiazines, related drugs competing for 3H-agonist indicative a D-2 dopamine receptor. Both agonist/3H-agonist antagonist/3H-agonist competition curves are monophasic noncooperative (nH =...
Abstract: A cDNA clone encoding a novel G protein‐linked receptor was isolated from rat cerebral cortex library using polymerase chain reaction‐amplified fragment as probe. This 2.4‐kb encodes 367 amino acid protein with seven putative transmembrane spanning domains. The is highly homologous to the cloned μ, δ, and κ opioid receptors shares them structural features such three glycosylation sites in terminus, cyclic AMP‐dependent kinase phosphorylation site third cytoplasmic loop, an aspartic...
Synaptic plasticity in the ventral tegmental area (VTA) has been implicated acquisition of a drug-dependent state. Even single exposure to cocaine naive animals is sufficient trigger sustained changes on VTA glutamatergic synapses that resemble activity-dependent long-term potentiation (LTP) other brain regions. However, an insight into its time course and mechanisms action limited. Here, we show acts locally within induce LTP-like enhancement AMPA receptor-mediated transmission not...