Substituted 3-benzazepine


A substituted 3-benzazepine, or simply 3-benzazepine, is a derivative of 3-benzazepine. They are cyclized phenethylamines and are closely related to the tetrahydroisoquinolines. In addition, they are analogous to the cyclized tryptamine ibogalogs and their β-carboline relatives.
3-Benzazepines are known to act as monoamine receptor modulators, including as dopamine D1-like receptor agonists, dopamine D1 receptor antagonists, and serotonin 5-HT2A, 5-HT2B, and 5-HT2C receptor agonists, among other activities. 3-Benzazepines acting as serotonin 5-HT2 receptor agonists generally show varying degrees of preferential activity at the serotonin 5-HT2C receptor over the serotonin 5-HT2A receptor, with occasional exceptions. One 3-benzazepine, the non-selective serotonin 5-HT2 receptor agonist and previously marketed anorectic lorcaserin, is known to produce psychedelic effects at supratherapeutic doses.

List of 3-benzazepines

StructureNameActionChemical nameRef
3-BenzazepineN/A3H-3-benzazepine
SKF-39315D1-like agonist2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol
Lorcaserin5-HT2 agonist-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine
7-Chlorolorcaserin5-HT2 agonist-7,8-dichloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine
SCHEMBL53343615-HT2 agonist7--2,3,4,5-tetrahydro-1H-3-benzazepine
SKF-38393D1-like agonist1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol
SKF-81297D1-like agonist-6-chloro-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol
FenoldopamD1-like agonist6-chloro-1--2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol
SCH-23390D1 antagonist-8-chloro-3-methyl-5-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-ol
SKF-83959D1-like agonist6-chloro-3-methyl-1--2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol
Trepipam D1-like agonist7,8-dimethoxy-3-methyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine
SKF-77434D1-like agonist-1-phenyl-3--2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol
SKF-82958D1-like agonist-6-chloro-1-phenyl-3--2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol
6-Br-APBD1-like agonist-6-bromo-1-phenyl-3--2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol
Odapipam D1 antagonist-8-chloro-5--3-methyl-1,2,4,5-tetrahydro-3-benzazepin-7-ol
Berupipam D1 antagonist-5--8-chloro-3-methyl-1,2,4,5-tetrahydro-3-benzazepin-7-ol
NNC 01-0687 D1 antagonist-5--3-methyl-8-nitro-1,2,4,5-tetrahydro-3-benzazepin-7-ol
GSK-189254H3 antagonist6--N-methylpyridine-3-carboxamide
Anilopam Opioid4-aniline

Related compounds

StructureNameActionChemical nameRef
PF-044797455-HT2 modulator-2-benzyl-N,9-dimethyl-6,7,8,9-tetrahydro-5H-pyrimidoazepin-4-amine
PF-047813405-HT2 modulator3-benzyl-N-methyl-6,7,8,9-tetrahydro-5H-pyridoazepin-1-amine