Psilocin, the active metabolite of psilocybin, is a psychedelic and agonist at the serotonin 2A receptor (5-HT2AR) that has shown positive therapeutic effects for brain disorders such as depression. To elucidate the brain effects of psilocybin, we directly compared the acute effects of 5-HT2...
The NTS1R agonist NT(8-13) reduces the G伪-mediated calcium signal in the NTS1R-DR complex compared to the NTS1R monomer which could be reversed by DR antagonists. The bivalent ligand CS148 (NTS1R-agonistic, DR-antagonistic) increased the calcium response addressing the dimer, consistent ...
[26]), the inverse agonist (IA) 1-methyl-4-[(5~{S})-3-methylsulfanyl-5,6-dihydrobenzo[b][1]benzothiepin-5-yl]piperazine (PDB ID: 6WH4 [25]), the 5-HT2AR partial antagonist (PA) and hallucinogen 25-CN-NBOH (PDB ID: 6WHA [25]), the 5-HT2AR agonist (3R)-3-methyl-5...
Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors. Significance for the modulation of frontocortical monoaminergic transmission and depressive ...
computational simulations of a serotonin 2A receptor (5-HT 2A R) model complexed with pharmacologically and structurally diverse ligands we identify different conformational states and dynamics adopted by the receptor bound to the full agonist 5-HT, the partial agonist LSD, and the inverse agonist ...
In the present studies, we tested the hypothesis that the psychedelic 5-HT2AR agonist R-(-)2,5-dimethoxy-4-iodoamphetamine (DOI) will decrease cocaine demand in a rodent behavioral economics model. Methods:Male, Sprague-Dawley rats (n = 28) were trained to self-administer cocaine (0.75 ...
A 5-HT2AR antagonist volinanserin was subcutaneously administrated 10 min before the 5-HT2AR agonist injection. Primary cortical neurons from embryos of female SD rats were cultured and used for assessing effects of 5-HT2AR agonists on neurite length. The necessity for 5-HT2AR stimulation ...
Mechanistically, we found that MNF or another β 2 -agonist zinterol markedly promoted heterodimerization of β 2 -ARs with 5-HT 2B Rs. Upregulation of the heterodimerized 5-HT 2B Rs and β 2 -ARs enhanced β 2 -AR-stimulated Gi-Akt signaling and cardioprotection while knockdown or ...
is to synthesis homodimeric 5-HT R antagonists, homodimeric 5-HTR agonists, and heterodimeric 5-HTR antagonist/5-HTR agonist that will exhibit improved ability to control cocaine induced behavior modifications compared to the concurrent administration of a 5-HTR antagonist and a 5-HTR agonist....
The effects of combined FGF2 and 5-HT agonist treatments on gamma oscillations point to a significant antagonistic interaction in astroglial FGFR1-5-HT1AR heterocomplexes that may contribute to counteraction of the 5-HT1AR-mediated decrease of gamma oscillations. This article is part of the special...