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1-(2'-Bromobenzyl)-6,7-dihydroxy- N -methyl-tetrahydroisoquinoline and 1,2-Demethyl-nuciferine as Agonists in Human D 2 Dopamine Receptors

Silva, Andrea G ; Vila, Laura ; Marques, Patrice ; Moreno, Laura ; Loza, Mabel ; Sanz, María-Jesús ; Cortes, Diego ; Castro, Marián ; Cabedo, Nuria

Journal of natural products (Washington, D.C.), 2020-01, Vol.83 (1), p.127-133 [Periódico revisado por pares]

United States

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Título:
1-(2'-Bromobenzyl)-6,7-dihydroxy- N -methyl-tetrahydroisoquinoline and 1,2-Demethyl-nuciferine as Agonists in Human D 2 Dopamine Receptors
Autor: Silva, Andrea G ; Vila, Laura ; Marques, Patrice ; Moreno, Laura ; Loza, Mabel ; Sanz, María-Jesús ; Cortes, Diego ; Castro, Marián ; Cabedo, Nuria
Assuntos: Animals ; Aporphines - chemistry ; Aporphines - pharmacology ; Cyclic AMP - chemistry ; Dopamine Agonists - chemistry ; Humans ; Isoquinolines - chemistry ; Molecular Structure ; Tetrahydroisoquinolines - chemistry ; Tetrahydroisoquinolines - pharmacology
É parte de: Journal of natural products (Washington, D.C.), 2020-01, Vol.83 (1), p.127-133
Descrição: Certain D -like dopamine receptor (DR) agonists are useful therapeutically as antiparkinsonian drugs, whereas D -like DR antagonists or partial agonists are proven effective as antipsychotics. Two isoquinoline derivatives, 1-(2'-bromobenzyl)-6,7-dihydroxy- -methyl-tetrahydroisoquinoline (Br-BTHIQ, ) and 1,2-demethyl-nuciferine (aporphine, ), were herein synthesized, and their dopaminergic affinity in cloned human D R, D R, and D R subtypes and their behavior as agonists/antagonists were evaluated. They showed affinity values ( ) for hD , hD , and hD DR within the nanomolar range. The trends in affinity were hD R ≫ hD R > hD R for Br-BTHIQ ( ) and hD R > hD R > hD R for 1,2-demethyl-nuciferine ( ). The functional assays of cyclic adenosine monophosphate signaling at human D R showed a partial agonist effect for Br-BTHIQ ( ) and full agonist behavior for aporphine ( ), with half maximal effective concentration values of 2.95 and 10.2 μM, respectively. Therefore, both isoquinolines and have emerged as lead molecules for the synthesis of new therapeutic drugs that ultimately may be useful to prevent schizophrenia and Parkinson's disease, respectively.
Editor: United States
Idioma: Inglês

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1-(2'-Bromobenzyl)-6,7-dihydroxy- N -methyl-tetrahydroisoquinoline and 1,2-Demethyl-nuciferine as Agonists in Human D 2 Dopamine Receptors

Silva, Andrea G ; Vila, Laura ; Marques, Patrice ; Moreno, Laura ; Loza, Mabel ; Sanz, María-Jesús ; Cortes, Diego ; Castro, Marián ; Cabedo, Nuria

United States

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