Modeling of ligand binding to dopamine D2 receptor
نویسندگان
چکیده
منابع مشابه
Modeling of ligand binding to the dopamine D2 receptor
The dopaminic receptors for a long time have been major targets for the development of new small molecules with high affinity and selectivity to treat psychiatric disorders, neurodegeneration, and drug abuse, and in other therapeutic areas. In the absence of a 3D structure for the human dopamine D2 (HDD2) receptor, the efforts for the discovery and design of new potential drugs rely on comparat...
متن کاملDopamine receptor D2
Dopamine receptor D2, also known asD2R, is a protein that, in humans, is encoded by the DRD2 gene.The dopamine D2 receptor was discovered in 1975 by Philip Seeman who had named it as the antipsychotic/dopamine receptor [1] The dopamine D2 receptor is the main receptor for all antipsychotic drugs. Any drug that does not interfere with dopamine action at the D2 receptor does not have an antipsych...
متن کاملReceptor, Ligand and Transducer Contributions to Dopamine D2 Receptor Functional Selectivity
Functional selectivity (or biased agonism) is a property exhibited by some G protein-coupled receptor (GPCR) ligands, which results in the modulation of a subset of a receptor's signaling capabilities and more precise control over complex biological processes. The dopamine D2 receptor (D2R) exhibits pleiotropic responses to the biogenic amine dopamine (DA) to mediate complex central nervous sys...
متن کاملModeling and mutational analysis of a putative sodium-binding pocket on the dopamine D2 receptor.
A homology model of the dopamine D2 receptor was constructed based on the crystal structure of rhodopsin. A putative sodium-binding pocket identified in an earlier model (PDB ) was revised. It is now defined by Asn-419 backbone oxygen at the apex of a pyramid and Asp-80, Ser-121, Asn-419, and Ser-420 at each vertex of the planar base. Asn-423 stabilizes this pocket through hydrogen bonds to two...
متن کاملDopamine D2 Receptor Dimer Formation
We have examined the binding of two radioligands ([H]spiperone and [H]raclopride) to D2 dopamine receptors expressed in Chinese hamster ovary cells. In saturation binding experiments in the presence of sodium ions, both radioligands labeled a similar number of sites, whereas in the absence of sodium ions [H]raclopride labeled about half the number of sites labeled by [H]spiperone. In competitio...
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ژورنال
عنوان ژورنال: Journal of the Serbian Chemical Society
سال: 2014
ISSN: 0352-5139,1820-7421
DOI: 10.2298/jsc130208046o