| Bioactivity | SB-222200 is a potent, selective, orally active and blood-brain barrier (BBB) penetrant NK-3 receptor antagonist. SB-222200 is developed for central nervous system (CNS) disorders[1]. | ||||||||||||
| Invitro | SB-222200 inhibits 125I-[MePhe7]neurokinin B (NKB) binding to CHO cell membranes stably expressing the hNK-3 receptor (CHO-hNK-3R) with a Ki of 4.4 nM[1].SB-222200 antagonizes NKB-induced Ca2+ mobilization in HEK 293 cells stably expressing the hNK-3 receptor (HEK 293-hNK-3R) with an IC50 of 18.4 nM[1].SB-222200 is selective for hNK-3 receptors compared with hNK-1 (Ki>100,000 nM) and hNK-2 receptors (Ki=250 nM)[1].SB-222200 (10 nM-1 μM) produces a concentration-dependent, surmountable inhibition of NKB-induced Ca2+ mobilization in HEK 293-hNK-3R cells[1]. | ||||||||||||
| In Vivo | SB-222200 (5 mg/kg; 30 min pretreatment) produces inhibition of behavioral responses induced by NK-3 receptor-selective agonist senktide (HY-P0187) in mice[1].SB-2222006 exhibits moderate oral bioavailability (rat 46%) and Cmax (rat 427 ng/mL) following oral administration (rat 10 mg/kg)[1].SB-2222006 exhibits terminal elimination half-life (rat 1.9 h) due to high plasma clearance (56 mL/min/kg) following intravenous administration (rat 2.5 mg/kg)[1]. Animal Model: | ||||||||||||
| Name | SB-222200 | ||||||||||||
| CAS | 174635-69-9 | ||||||||||||
| Formula | C26H24N2O | ||||||||||||
| Molar Mass | 380.48 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Sarau HM, et al. Nonpeptide tachykinin receptor antagonists. II. Pharmacological and pharmacokinetic profile of SB-222200, a central nervous system penetrant, potent and selective NK-3 receptor antagonist. J Pharmacol Exp Ther. 2000 Oct;295(1):373-81. |