Big Chemical Encyclopedia

Chemical substances, components, reactions, process design ...

Articles Figures Tables About

Serotonin ligands

Glennon RA et al. (1988) Arylpiperazine derivatives as high-affinity 5-HTlA serotonin ligands. J Med Chem 31(10) 1968-1971... [Pg.96]

Kunovac JL, Stahl SM Biochemical pharmacology of serotonin receptor subtypes hypothesis for clinical applications of selective serotonin ligands. International Review of Psychiatry 7 55-67, 1995... [Pg.677]

Enterochromaffin cells are interspersed with mucosal cells mainly in the stomach and small intestine. In the blood, serotonin is present at high concentrations in platelets, which take up serotonin from the plasma by an active transport process. Serotonin is released on platelet activation. In the central nervous system, serotonin serves as a transmitter. The main serotonin-containing neurons are those clustered in form of the Raphe nuclei. Serotonin exerts its biological effects through the activation of specific receptors. Most of them are G-protein coupled receptors (GPCRs) and belong to the 5-HTr, 5-HT2-, 5-HT4-, 5-HTs-, 5-HT6-, 5-HT7-receptor subfamilies. The 5-HT3-receptor is a ligand-operated ion channel. [Pg.1120]

Recent evidence indicates that the 5-HT transporter is subject to post-translational regulatory changes in much the same way as neurotransmitter receptors (Blakeley et al. 1998). Protein kinase A and protein kinase C (PKC), at least, are known to be involved in this process. Phosphorylation of the transporter by PKC reduces the Fmax for 5-HT uptake and leads to sequestration of the transporter into the cell, suggesting that this enzyme has a key role in its intracellular trafficking. Since this phosphorylation is reduced when substrates that are themselves transported across the membrane bind to the transporter (e.g. 5-HT and fi -amphetamine), it seems that the transport of 5-HT is itself linked with the phosphorylation process. Possibly, this process serves as a homeostatic mechanism which ensures that the supply of functional transporters matches the demand for transmitter uptake. By contrast, ligands that are not transported (e.g. cocaine and the selective serotonin reuptake inhibitors (SSRIs)) prevent the inhibition of phosphorylation by transported ligands. Thus, such inhibitors would reduce 5-HT uptake both by their direct inhibition of the transporter and by disinhibition of its phosphorylation (Ramamoorthy and Blakely 1999). [Pg.195]

Arylpiperazines have immensely important effects on various and diverse biological targets, in particular on CNS receptors. In the case of serotonin (5-HT) receptors, compounds containing this arylpiperazine moiety represent the largest systematically studied class of 5-HTia receptor ligands [63]. Structural alterations within long-chain arylpiperazines (LCAPs) occur mainly at the two opposite ends of a molecule and have been described by many authors [64-71]. [Pg.89]

The affinity (Kj values) observed for [ H]MDA and [ HJMDMA binding were similar to the effective doses (i.e., ED50 or K] values) of MDA and MDMA reported for various pre- and postsynaptic monoamine markers, such as serotonin and dopamine release (Johnson et al. 1986), monoamine transport (Steele et al. 1987), and multiple brain, ligand binding sites (Battaglia et al. 1988). [Pg.225]

The authors also identified the most common structural motifs unique to ligands of individual classes of GPCRs such as the adrenergic, dopamine, histamine, muscarinic, and serotonin receptors as shown in Table 1. [Pg.413]

Three families of serotonin receptor, the 5-HT family, the 5-HT2 family and the family that includes the 5-HT4, 5-ht6 and 5-HT7 receptors represent the three major classes of 5-HT receptor that are G-protein-coupled receptors (Ch. 19). The 5-HT3 receptor is a ligand-gated ion channel and is a separate family. Although each serotonin receptor can be potently activated by 5-HT, differences insignal transduction mechanisms,neuroanatomical distribution and affinities for synthetic chemicals create opportunities for drug discovery and make each 5-HT receptor subtype a potential therapeutic target. [Pg.241]

Barker, E. L., Kimmel, H. L., and Blakely, R. D. (1994) Chimeric human and rat serotonin transporters reveal domains involved in recognition of transporter ligands. Mol. Pharmacol. 46, 799-807. [Pg.208]

Ebersole, B. J., Visiers, I., Weinstein, H., and Sealfon, S. (2003) Molecular basis of partial agonism orientation of indolamine ligands in the binding pocket of the human serotonin 5-HT2A receptor determines relative efficacy. Mol. Pharmacol. 63, 36—43. [Pg.255]

Choudhary, M. S., Craigo, S., and Roth, B. L. (1992) Identification of receptor domains that modify ligand binding to 5-hydroxytryptamine2 and 5-hydroxytryptaminelC serotonin receptors. Mol. Pharmacol. 42, 627-633. [Pg.257]

Mehl, E., Riither, E., and Redemann, J. (1977) Endogenous ligands of a putative LSD-serotonin receptor in the cerebrospinal fluid Higher level of LSD-displacing factors (LDF) in unmedicated psychotic patients. Psychopharmacology, 54 9-16. [Pg.90]


See other pages where Serotonin ligands is mentioned: [Pg.133]    [Pg.185]    [Pg.133]    [Pg.185]    [Pg.517]    [Pg.201]    [Pg.150]    [Pg.77]    [Pg.560]    [Pg.1120]    [Pg.1120]    [Pg.1172]    [Pg.1237]    [Pg.283]    [Pg.195]    [Pg.412]    [Pg.246]    [Pg.100]    [Pg.60]    [Pg.100]    [Pg.112]    [Pg.117]    [Pg.265]    [Pg.117]    [Pg.168]    [Pg.294]    [Pg.165]    [Pg.236]    [Pg.241]    [Pg.261]    [Pg.890]    [Pg.895]    [Pg.947]    [Pg.947]    [Pg.954]    [Pg.117]    [Pg.107]    [Pg.96]    [Pg.241]    [Pg.202]   
See also in sourсe #XX -- [ Pg.369 , Pg.370 ]




SEARCH



Serotonin receptor ligands

© 2024 chempedia.info