Mach, Ulrich R.; Hackling, Anneke E.; Perachon, Sylvie; Ferry, Sandrine; Wermuth, Camille G.; Schwartz, Jean-Charles; Sokoloff, Pierre; Stark, Holger published the artcile< Development of novel 1,2,3,4-tetrahydroisoquinoline derivatives and closely related compounds as potent and selective dopamine D3 receptor ligands>, Recommanded Product: 1,2,3,4-Tetrahydroisoquinolin-5-amine, the main research area is tetrahydroisoquinoline derivative dopamine D3 receptor ligand.
Based on N-alkylated 1,2,3,4-tetrahydroisoquinoline derivatives which are structurally related to the partial agonist BP 897, a series of novel, selective dopamine D3 receptor antagonists has been synthesized. Derivatization included changes in the arylamide moiety and the tetrahydroisoquinoline substructure leading to compounds with markedly improved selectivities and affinities in the low nanomolar concentration range. From the 55 structures presented here, (E)-3-(4-iodophenyl)-N-(4-(1,2,3,4-tetrahydroisoquinolin-2-yl)butyl)acrylamide (51) has high affinity (Ki(hD3) = 12 nM) and a 123-fold preference for the D3 receptor relative to the D2 receptor subtype. Its pharmacol. profile offers the prospect of a novel radioligand as a tool for various dopamine D3-receptor-related in vitro and in vivo investigations.
ChemBioChempublished new progress about Dopamine D3 receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 115955-90-3 belongs to class tetrahydroisoquinoline, and the molecular formula is C9H12N2, Recommanded Product: 1,2,3,4-Tetrahydroisoquinolin-5-amine.
Referemce:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem