149355-52-2, Name is 1,2,3,4-Tetrahydroisoquinoline-7-carbonitrile, belongs to tetrahydroisoquinoline compound, is a common compound. COA of Formula: C10H10N2In an article, once mentioned the new application about 149355-52-2.
Design and synthesis of trans-N-[4-[2-(6-cyano-1,2,3,4- tetrahydroisoquinolin-2-yl)ethyl]cyclohexyl]-4-quinolinecarboxamide (SB- 277011): A potent and selective dopamine D3 receptor antagonist with high oral bioavailability and CNS penetration in the rat
A selective dopamine D3 receptor antagonist offers the potential for an effective antipsychotic therapy, free of the serious side effects of currently available drugs. Using clearance and brain penetration studies as a screen, a series of 1,2,3,4-tetrahydroisoquinolines, exemplified by 13, was identified with high D3 affinity and selectivity against the D2 receptor. Following examination of molecular models, the flexible butyl linker present in 13 was replaced by a more conformationally constrained cyclohexylethyl linker, leading to compounds with improved oral bioavailability and selectivity over other receptors. Subsequent optimization of this new series to improve the cytochrome P450 inhibitory profile and CNS penetration gave trans-N[4-[2-(6-cyano-1,2,3,4-tetrahydroisoquinolin-2-yl)ethyl]cyclohexyl]-4- quinolinecarboxamide (24, SB-277011). This compound is a potent and selective dopamine D3 receptor antagonist with high oral bioavailability and brain penetration in the rat and represents an excellent new chemical tool for the investigation of the role of the dopamine D3 receptor in the CNS.
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Reference：
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem