Drug intelligence / Profile preview

1,2,3,4-tetrahydroisoquinoline-7-sulfonamide

Development stage
Preclinical
Lead developer
GSK
Modality
Small Molecules
01

Overview

1,2,3,4-tetrahydroisoquinoline-7-sulfonamide is a synthetic small molecule featuring a tetrahydroisoquinoline core with a sulfonamide group at the 7-position. It is primarily recognized as a selective inhibitor of phenylethanolamine N-methyltransferase (PNMT), an enzyme responsible for converting norepinephrine to epinephrine in the adrenal medulla. By inhibiting PNMT activity through binding in an aromatic-rich non-conserved pocket of the enzyme (enabling hydrogen bonding and π–π interactions), this compound can modulate adrenaline biosynthesis and influence stress response and cardiovascular pathways. While it has not been approved for clinical use or advanced beyond experimental research stages as of June 2025[1][5], it remains valuable in pharmacological studies exploring catecholamine metabolism and related biological processes.

Other names
1,2,3,4-Tetrahydro-Isoquinoline-7-Sulfonic Acid AmideTHIQ-7-SATHIQ7-SATHIQ 7-SA
02

Targets

PNMT (Phenylethanolamine N-methyltransferase)

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