Results 21 to 30 of about 2,277 (153)

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

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

Aromatic linker variations in novel dopamine D2 and D3 receptor ligands

Archiv der Pharmazie, Volume 357, Issue 8, August 2024.
Within the blueprint motifs of dopamine D2R/D3R ligands, the butyl (tetramethylene) linker was replaced by substituted benzyl or phenethyl linkers, maintaining high affinities at both receptor subtypes. Abstract Dopamine D2‐like receptors, especially D2 and D3 receptor subtypes, are important targets of antipsychotic agents.
Cristian Di Biase, Luisa Leitzbach, Annika Frank, Aleksandra Zivkovic, Holger Stark   +4 more
wiley   +1 more source

Discovery of a Small Molecule Activator of Slack (Kcnt1) Potassium Channels That Significantly Reduces Scratching in Mouse Models of Histamine‐Independent and Chronic Itch

Advanced Science, Volume 11, Issue 15, April 17, 2024.
The potassium channel Slack is highly expressed in sensory neurons that sense itch. In this study, several new compounds that activate Slack are developed. It is found that the lead molecule, compound 6, effectively inhibits scratching elicited by multiple pruritogens in mice establishing Slack activation as a novel pharmacological strategy for the ...
Annika Balzulat, W. Felix Zhu, Cathrin Flauaus, Victor Hernandez‐Olmos, Jan Heering, Sunesh Sethumadhavan, Mariam Dubiel, Annika Frank, Amelie Menge, Maureen Hebchen, Katharina Metzner, Ruirui Lu, Robert Lukowski, Peter Ruth, Stefan Knapp, Susanne Müller, Dieter Steinhilber, Inga Hänelt, Holger Stark, Ewgenij Proschak, Achim Schmidtko   +20 more
wiley   +1 more source

Anxious‐depressive attack and rejection sensitivity—Toward a new approach to treatment‐resistant depression

Neuropsychopharmacology Reports, Volume 44, Issue 1, Page 17-28, March 2024.
The structural equation model of the relationships between rejectionsensitivity (RS) and anxious‐depressive attack (ADA). RS contributes significantly to the onset of ADA. Abstract This paper aimed to find clues to treatment‐resistant depression (TRD) solutions.
Hisanobu Kaiya
wiley   +1 more source

Effects of chronic haloperidol treatment on the expression of fear memory and fear memory extinction in the cued fear‐conditioned rats

Neuropsychopharmacology Reports, Volume 44, Issue 1, Page 197-205, March 2024.
Chronic haloperidol impacts fear memory differently than single doses. Our study unveils how chronic D2R antagonist treatment alters fear memory expression and extinction in rats, offering crucial insights into potential therapeutic approaches for fear memory disorders.
Kosuke Enomoto, Kazuro Shibata, Hiroyuki Muraoka, Masahiko Kawano, Ken Inada, Jun Ishigooka, Katsuji Nishimura, Hidehiro Oshibuchi   +7 more
wiley   +1 more source

Inhibition of Cutaneous Contact Hypersensitivity in the Mouse with Systemic or Topical Spiperone: Topical Application of Spiperone Produces Local Immunosuppression Without Inducing Systemic Neuroleptic Effects

Journal of Investigative Dermatology, 1992
We tested the ability of the neuroleptic agent spiperone (8-[3-(p-fluorobenzoyl)propyl]-1-phenyl-1,3,8-triazaspiro-[4.5] decan-4- one) to influence the tissue swelling and leukocyte infiltration associated with T-cell--dependent immune responses, i.e., contact hypersensitivity reactions, in mice.
Akila Chandrasekar, Richard J. Sharpe, Zheng-Sheng. Wang, Stephen J. Galli, Kenneth A. Arndt   +4 more
openaire   +3 more sources

Fluorescent Tools for the Imaging of Dopamine D2‐Like Receptors**

ChemBioChem, Volume 25, Issue 2, January 15, 2024.
In this study, we have identified UR‐MN212 (20), a spiperone‐based fluorescent ligand bearing a 5‐TAMRA dye, as suitable for fluorescence microscopy at the D2R. The binding affinity in the single‐digit nanomolar range could be determined in radioligand competition binding and molecular brightness studies at D2‐like receptors.
Martin Nagl, Denise Mönnich, Niklas Rosier, Hannes Schihada, Alexei Sirbu, Nergis Konar, Irene Reyes‐Resina, Gemma Navarro, Rafael Franco, Peter Kolb, Paolo Annibale, Steffen Pockes   +11 more
wiley   +1 more source

High intensity interval training exercise increases dopamine D2 levels and modulates brain dopamine signaling. [PDF]

Front Public Health, 2023
Tyler J, Podaras M, Richardson B, Roeder N, Hammond N, Hamilton J, Blum K, Gold M, Baron DA, Thanos PK.   +9 more
europepmc   +1 more source

Ovarian Steroids Modulate the Release of Dopamine into Hypophysial Portal Blood and the Density of Anterior Pituitary [³H]Spiperone-Binding Sites in Ovariectomized Rats* [PDF]

, 1984
Nancy S. Pilotte, David R. Burt, Charles A. Barraclough   +2 more
openalex   +1 more source