Results 31 to 40 of about 4,488 (204)

Synthesis of novel 2-(piperazino-1-yl-alkyl)-1H-benzimidazole derivates and assessment of their interactions with the D2 dopamine receptor [PDF]

Journal of the Serbian Chemical Society, 2019
A total of 14 novel arylpiperazines were synthesized, and pharmacologically evaluated by measuring their affinities towards the D2 dopamine receptor (DRD2) in a [3H]spiperone competition assay.
Penjišević Jelena Z., Andrić Deana B., Šukalović Vladimir B., Roglić Goran M., Šoškić Vukić, Kostić-Rajačić Slađana V.   +5 more
doaj   +1 more source

Transcriptome‐based insights into gene networks controlling myopia prevention

The FASEB Journal, Volume 35, Issue 9, September 2021., 2021
Abstract Myopia (short‐sightedness), usually caused by excessive elongation of the eye during development, has reached epidemic proportions worldwide. In animal systems including the chicken model, several treatments have been shown to inhibit ocular elongation and experimental myopia.
Cindy Karouta, Robert Kucharski, Kristine Hardy, Kate Thomson, Ryszard Maleszka, Ian Morgan, Regan Ashby   +6 more
wiley   +1 more source

Spatial intensity distribution analysis: studies of G Protein-coupled receptor oligomerization [PDF]

, 2018
Spatial intensity distribution analysis (SpIDA) is a recently developed approach for determining quaternary structure information on fluorophore-labelled proteins of interest in situ. It can be applied to live or fixed cells and native tissue.
Marsango, Sara, Milligan, Graeme, Pediani, John D., Ward, Richard J.   +3 more
core   +1 more source

Pharmacology of Drugs Used as Stimulants

The Journal of Clinical Pharmacology, Volume 61, Issue S2, Page S53-S69, August 2021., 2021
Abstract Psychostimulant, cardiovascular, and temperature actions of stimulants involve adrenergic (norepinephrine), dopaminergic (dopamine), and serotonergic (serotonin) pathways. Stimulants such as amphetamine, 3,4‐methylenedioxymethamphetamine (MDMA), or mephedrone can act on the neuronal membrane monoamine transporters NET, DAT, and SERT and/or the
James R. Docherty, Hadeel A. Alsufyani
wiley   +1 more source

Enhanced tyrosine hydroxylase activity induces oxidative stress, causes accumulation of autotoxic catecholamine metabolites, and augments amphetamine effects in vivo

Journal of Neurochemistry, Volume 158, Issue 4, Page 960-979, August 2021., 2021
This paper investigates the effect of increased activity of tyrosine hydroxylase (TH), the rate‐limiting enzyme in catecholamine synthesis, in a novel line of TH over‐expressing mice. Past studies suggest that in synucleinopathies, early pathological changes can result in decreased TH regulation and increased activity.
Laura M. Vecchio, Patricia Sullivan, Amy R. Dunn, Marie Kristel Bermejo, Rong Fu, Shababa T. Masoud, Emil Gregersen, Nikhil M. Urs, Reza Nazari, Poul Henning Jensen, Amy Ramsey, David S. Goldstein, Gary W. Miller, Ali Salahpour   +13 more
wiley   +1 more source

Cabergoline, dopamine D2 receptor agonist, prevents neuronal cell death under oxidative stress via reducing excitotoxicity. [PDF]

PLoS ONE, 2014
Several lines of evidence demonstrate that oxidative stress is involved in the pathogenesis of neurodegenerative diseases, including Parkinson's disease. Potent antioxidants may therefore be effective in the treatment of such diseases.
Haruki Odaka, Tadahiro Numakawa, Naoki Adachi, Yoshiko Ooshima, Shingo Nakajima, Yusuke Katanuma, Takafumi Inoue, Hiroshi Kunugi   +7 more
doaj   +1 more source

Cardiovascular and temperature adverse actions of stimulants

British Journal of Pharmacology, Volume 178, Issue 13, Page 2551-2568, July 2021., 2021
The vast majority of illicit stimulants act at monoaminergic systems, causing both psychostimulant and adverse effects. Stimulants can interact as substrates or antagonists at the nerve terminal monoamine transporter that mediates the reuptake of monoamines across the nerve synaptic membrane and at the vesicular monoamine transporter (VMAT‐2) that ...
James R. Docherty, Hadeel A. Alsufyani
wiley   +1 more source

Fast phasic release properties of dopamine studied with a channel biosensor [PDF]

, 2014
Few other neurotransmitters are of as intense interest to neuropsychiatry and neurology as dopamine, yet existing techniques to monitor dopamine release leave an important spatiotemporal gap in our understanding. Electrochemistry and fluorescence imaging
Benz, Ann, Harmon, Steve, Kress, Geraaldine J, Mennerick, Steven, Shu, Hong-Jin, Taylor, Amanda, Yu, Andrew   +6 more
core   +2 more sources

Dopamine D_2-receptor activation elicits akinesia, rigidity, catalepsy, and tremor in mice expressing hypersensitive 4 nicotinic receptors via a cholinergic-dependent mechanism [PDF]

, 2010
Recent studies suggest that high-affinity neuronal nicotinic acetylcholine receptors (nAChRs) containing α4 and β2 subunits (α4β2*) functionally interact with G-protein-coupled dopamine (DA) D_2 receptors in basal ganglia.
Andrew R. Tapper, Bruce N. Cohen, Coward D. M., Franklin K. B. J., Henry A. Lester, Herwig Just, Janssen P. A., Lester H. A., Mercuri N. B., Outi Salminen, Paul D. Gardner, Paul Whiteaker, Raz A., Rubing Zhao-Shea, Salminen O., Sharon R. Grady, Sotnikova T. D., Tapper A. R., Tristan McClure-Begley   +18 more
core   +3 more sources

The role of kinetic context in apparent biased agonism at GPCRs [PDF]

, 2016
Biased agonism describes the ability of ligands to stabilize different conformations of a GPCR linked to distinct functional outcomes and offers the prospect of designing pathway-specific drugs that avoid on-target side effects. This mechanism is usually
A Akinc, A Hill, A Lahti, A Saulière, AW Kahsai, B Masri, C Sampaio, D Guo, D Möller, D Sykes, D Unett, D Wacker, DA Sykes, DR Sibley, EJ Whalen, ET van der Westhuizen, F Pedregosa, GJ Kilpatrick, H Abdi, H Motulsky, H Sheth, J Allen, J McPherson, J Shonberg, J Shonberg, JD Urban, JD Urban, JD Violin, JE Murphy, JJ Liu, JP Overington, JP Vilardaga, JR Lane, JW Black, JW Wisler, KV Andreassen, L Carboni, L Gazi, M Griffin, M Szabo, M Vilums, MT Drake, N Tschammer, O Agid, P Molinari, P Tummino, R Irannejad, R Rahmeh, S Ahn, S Durgam, S Ferrandon, S Galandrin, S Nijmeijer, S Rajagopal, SJ Charlton, SK Shenoy, T Kenakin, T Kenakin, T Kenakin, T Warne, W Stallaert, X-T Chen, Y Cheng   +62 more
core   +1 more source