| Name | SB-222200 |
| Description | SB-222200 is a selective, reversible, and competitive antagonist of the human NK-3 receptor(Ki=4.4 nM). |
| In vitro | SB-222200 inhibited (125)I-[MePhe(7)]neurokinin B (NKB) binding to Chinese hamster ovary (CHO) cell membranes stably expressing the hNK-3 receptor (CHO-hNK-3R) with a K(i) = 4.4 nM and antagonized NKB-induced Ca(2+) mobilization in HEK 293 cells stably expressing the hNK-3 receptor (HEK 293-hNK-3R) with an IC(50) = 18.4 nM. SB-222200 was selective for hNK-3 receptors compared with hNK-1 (K(i) > 100,000 nM) and hNK-2 receptors (K(i) = 250 nM). n HEK 293 cells transiently expressing murine NK-3 receptors (HEK 293-mNK-3R), SB-222200 inhibited binding of (125)I-[MePhe(7)]NKB (K(i) = 174 nM) and antagonized NKB (1 nM)-induced calcium mobilization (IC(50) = 265 nM) [1]. |
| In vivo | In mice, oral administration of SB-222200 produced dose-dependent inhibition of behavioral responses induced by i.p. or intracerebral ventricular administration of the NK-3 receptor-selective agonist, senktide, with ED(50) values of approximately 5 mg/kg. SB-222200effectively crossed the blood-brain barrier in the mouse and rat. The inhibitory effect of SB-222200 against senktide-induced behavioral responses in the mouse correlated significantly with the brain, but not plasma, concentrations of the compound. Pharmacokinetic evaluation of SB-222200 in rat after oral administration (8 mg/kg) indicated sustained plasma concentrations (C(max) = about 400 ng/ml) and bioavailability of 46% [1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 100 mg/mL (262.83 mM)
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| Keywords | NKB | NK-3R | NK receptor | SB222200 | penetrant | inhibit | CNS | Neurokinin Receptor | Tachykinin receptor | nervous | central | SB-222200 | system | Inhibitor | SB 222200 | neurokinin-B | disorders |
| Inhibitors Related | Lanepitant 2HCl | Rolapitant | Ezlopitant | (R)-CJ 11974 | N-Acetyl-L-tryptophan | Netupitant | Aprepitant | Vofopitant dihydrochloride | Befetupitant | Vofopitant | Fosaprepitant dimeglumine | Maropitant |
| Related Compound Libraries | Bioactive Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | CNS-Penetrant Compound Library | Inhibitor Library | NO PAINS Compound Library | Orally Active Compound Library | Bioactive Compounds Library Max | GPCR Compound Library |
United States
