Trazpiroben (TAK-906) is a potent, peripherally selective D2/D3 dopamine receptor antagonist, moderate affinity for D4, and minimal for D1 and D5.
Trazpiroben demonstrated the following receptor affinities: high for D2 and D3, moderate for D4, and minimal for D1 and D5, showed moderate affinity for adrenergic α 1B (α 1B) and 5HT)2A receptors and low potential for off-target adverse events (AEs).
Trazpiroben potently inhibited dopamine-activated D2L receptor activation of cognate G-proteins in human embryonic kidney 293 cell membranes and was a neutral D2L receptor antagonist.
Trazpiroben dose-dependently increased prolactin release in orally dosed rat (0.1-1 mg/kg).
Trazpiroben is a potent D2/D3 receptor antagonist designed to avoid the serious potential AEs associated with current gastroparesis.therapies.
Physicochemical Properties
M.Wt
633.742
Formula
C35H43N3O8
Appearance
Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility
10 mM in DMSO
Chemical Name/SMILES
3-((1-cyclohexyl-4-oxo-8-(4-oxo-4-phenylbutyl)-1,3,8-triazaspiro[4.5]decan-3-yl)methyl)benzoic acid compound with maleic acid (1:1)
