Results 1 to 10 of about 474 (115)

Inverse Agonist Activity of Sarpogrelate, a Selective 5-HT2A-Receptor Antagonist, at the Constitutively Active Human 5-HT2A Receptor

Journal of Pharmacological Sciences, 2006
Mutations producing constitutively active G-protein coupled receptors have been found in the pathophysiology of several diseases, implying that inverse agonists at the constitutively active receptors may have preferred therapeutic applications.
Habib Abul Muntasir, Mohiuddin Ahmed Bhuiyan, Masaji Ishiguro, Masanobu Ozaki, Takafumi Nagatomo   +4 more
doaj   +8 more sources

Identification of 5-HT2A receptor signaling pathways associated with psychedelic potential

Nature Communications, 2023
Serotonergic psychedelics possess considerable therapeutic potential. Although 5-HT2A receptor activation mediates psychedelic effects, prototypical psychedelics activate both 5-HT2A-Gq/11 and β-arrestin2 transducers, making their respective roles ...
Jason Wallach, Andrew B. Cao, Maggie M. Calkins, Andrew J. Heim, Janelle K. Lanham, Emma M. Bonniwell, Joseph J. Hennessey, Hailey A. Bock, Emilie I. Anderson, Alexander M. Sherwood, Hamilton Morris, Robbin de Klein, Adam K. Klein, Bruna Cuccurazzu, James Gamrat, Tilka Fannana, Randy Zauhar, Adam L. Halberstadt, John D. McCorvy   +18 more
doaj   +1 more source

PACAP–PAC1 Signaling Regulates Serotonin 2A Receptor Internalization

Frontiers in Endocrinology, 2021
Mice lacking pituitary adenylate cyclase-activating polypeptide (PACAP) display psychomotor abnormalities, most of which are ameliorated by atypical antipsychotics with serotonin (5-HT) 2A receptor (5-HT2A) antagonism. Heterozygous Pacap mutant mice show
Atsuko Hayata-Takano, Atsuko Hayata-Takano, Yusuke Shintani, Keita Moriguchi, Naoki Encho, Kohei Kitagawa, Takanobu Nakazawa, Takanobu Nakazawa, Hitoshi Hashimoto, Hitoshi Hashimoto, Hitoshi Hashimoto, Hitoshi Hashimoto, Hitoshi Hashimoto   +12 more
doaj   +1 more source

Serotonin 5-HT2A receptor activity mediates adipocyte differentiation through control of adipogenic gene expression

Scientific Reports, 2021
Serotonin 5-HT2 receptors are expressed in many tissues and play important roles in biological processes. Although the 5-HT2A receptor is primarily known for its role in central nervous system, it is also expressed in peripheral tissues.
Bangning Yu, Diana M. Battaglia, Timothy P. Foster, Charles D. Nichols   +3 more
doaj   +1 more source

St. John's wort extract STW3-VI affects the binding behaviour, signal transduction and lateral mobility of 5-HT2A receptors observed by single molecule detection and the use of a novel fluorescence-labeled ligand

Phytomedicine Plus, 2022
Background: 5-HT2A receptors play an important role in the development and therapy of depression. St. John's wort (SJW) extracts are used in the treatment of depression.
Stefan Aatz, Sebastian Franken, Christiane Kolb, Hanns Häberlein   +3 more
doaj   +1 more source

Human Cortical Serotonin 2A Receptor Occupancy by Psilocybin Measured Using [11C]MDL 100,907 Dynamic PET and a Resting-State fMRI-Based Brain Parcellation

Frontiers in Neuroergonomics, 2022
Psilocybin (a serotonin 2A, or 5-HT2A, receptor agonist) has shown preliminary efficacy as a treatment for mood and substance use disorders. The current report utilized positron emission tomography (PET) with the selective 5-HT2A receptor inverse agonist
Frederick S. Barrett, Frederick S. Barrett, Yun Zhou, Theresa M. Carbonaro, Joshua M. Roberts, Gwenn S. Smith, Gwenn S. Smith, Roland R. Griffiths, Roland R. Griffiths, Dean F. Wong   +9 more
doaj   +1 more source

Receptor Interaction Profiles of 4-Alkoxy-3,5-Dimethoxy-Phenethylamines (Mescaline Derivatives) and Related Amphetamines

Frontiers in Pharmacology, 2022
3,4,5-Trimethoxyphenethylamine (mescaline) is a psychedelic alkaloid found in peyote cactus. Related 4-alkoxy-3,5-dimethoxy-substituted phenethylamines (scalines) and amphetamines (3C-scalines) are reported to induce similarly potent psychedelic effects ...
Karolina E. Kolaczynska, Dino Luethi, Dino Luethi, Daniel Trachsel, Marius C. Hoener, Matthias E. Liechti   +5 more
doaj   +1 more source

The serotonin receptor 5-HT2A modulates lifespan and protein feeding in Drosophila melanogaster

Frontiers in Aging, 2022
The conserved neurotransmitter serotonin has been shown to be an important modulator of lifespan in specific nutritional contexts; however, it remained unclear how serotonin signaling influences lifespan under normal conditions.
Allyson S. Munneke, Tuhin S. Chakraborty, Saige S. Porter, Christi M. Gendron, Scott D. Pletcher, Scott D. Pletcher, Scott D. Pletcher   +6 more
doaj   +1 more source

Serotonergic signals enhanced hamster sperm hyperactivation

The Journal of Reproduction and Development, 2021
In the present study, we investigated the regulatory mechanisms underlying sperm hyperactivation enhanced by 5-hydroxytryptamine (5-HT) in hamsters. First, we examined the types of 5-HT receptors that regulate hyperactivation.
Chiyori SAKAMOTO, Masakatsu FUJINOKI, Masafumi KITAZAWA, Satoshi OBAYASHI   +3 more
doaj   +1 more source

Characterization of the human 5-HT2A receptor gene promoter [PDF]

The Journal of Neuroscience, 1995
The regulation of 5-HT2A receptor (5-HT2AR) expression has been implicated in a variety of pathological processes and has been shown to be extremely complicated and controversial. In order to understand the mechanisms of regulation of this receptor, it is important to characterize its promoter.
Q S, Zhu, K, Chen, J C, Shih
openaire   +2 more sources