S-Isopropylisothiourea (hydrobromide)

S-Isopropylisothiourea hydrobromide (S-isopropyl ITU; IPTU) is a blood-brain barrier (BBB) penetrant NOS inhibitor with IC₅₀ values of 0.66, 0.75 and 0.29 μM against mouse spinal cord, cerebellar, bovine aortic and porcine endothelial cell NOS. S-Isopropylisothiourea exhibits a significant blood pressure-raising effect without damaging the perfusion of vital organs and can also inhibit the late-phase pain response induced by formalin. S-Isopropylisothiourea hydrobromide is used in the researchs for hemorrhagic shock and pain response based on NOS^[1][2]. In Vivo:S-Isopropylisothiourea hydrobromide (50 mg/kg, i.p., single dose) can pass through the blood-brain barrier and reach an effective concentration in the central nervous system, and achieves a potent and sustained blood-pressure-raising effect by inhibiting vascular eNOS in mice^[1].
S-Isopropylisothiourea hydrobromide (10-50 mg/kg, i.p., single dose) exhibits selective analgesic effects at a dose of 50 mg/kg, specifically inhibiting pain in the late phase (15-30 min)^[1].
S-Isopropylisothiourea hydrobromide (0.1 mg/kg, i.v., 3 doses) significantly increases mean arterial pressure (MAP) and achieve a 100% survival rate in a rat model of severe hemorrhagic shock^[2].
S-Isopropylisothiourea hydrobromide (0.3 mg/kg plus 1 mg/kg·h, i.v., maintain infusion for 120 min) significantly increases MAP to a normal level, without reducing cardiac output, and maintain perfusion of vital organs^[2].