174635-69-9
174635-69-9 結(jié)構(gòu)式
基本信息
SB 222200
SB-222200
SB222200
(S)-3-METHYL-2-PHENYL-N-(1-PHENYLPROPYL)-4-QUINOLINECARBOXAMIDE
3-Methyl-2-phenyl-N-((1S)-1-phenylpropyl)quinoline-4-carboxamide
3-METHYL-2-PHENYL-N-[(1S)-1-PHENYLPROPYL]-4-QUINOLINECARBOXAMIDE
4-Quinolinecarboxamide, 3-methyl-2-phenyl-N-[(1S)-1-phenylpropyl]-
SB222200//3-Methyl-2-phenyl-N-[(1S)-1-phenylpropyl]quinoline-4-carboxaMide
物理化學(xué)性質(zhì)
常見問題列表
|
NK3
|
SB-222200 inhibits
125
I-[MePhe
7
]neurokinin B (NKB) binding to CHO cell membranes stably expressing the hNK-3 receptor (CHO-hNK-3R) with a K
i
of 4.4 nM and antagonizes NKB-induced Ca
2+
mobilization in HEK 293 cells stably expressing the hNK-3 receptor (HEK 293-hNK-3R) with an IC
50
of 18.4 nM.
SB-222200 is selective for hNK-3 receptors compared with hNK-1 (K
i
>100,000 nM) and hNK-2 receptors (K
i
=250 nM).
SB-222200 (10 nM-1 μM) produces a concentration-dependent, surmountable inhibition of NKB-induced Ca
2+
mobilization in HEK 293-hNK-3R cells.
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.
SB-222200 exhibits terminal elimination half-lives (rat about 2 h) and high systemic plasma clearance (56 mL/min/kg), with a moderately large volume of distribution (3-5 L/kg).
| Animal Model: | Male BALB/c mice (19-21 g) |
| Dosage: | 5 mg/kg |
| Administration: | Oral administration |
| Result: | Produced 57% inhibition of senktide-induced behavioral responses in mice. |
| Animal Model: | Male Sprague-Dawley rats (300-400 g) |
| Dosage: | 2.5 mg/kg for i.v.; 10 mg/kg for p.o. (Pharmacokinetic Analysis) |
| Administration: | Intravenous injection and oral gavage |
| Result: | Oral bioavailability (46%), T 1/2 (2.4 h for i.v.; 2.1 h for p.o.), C max (427 ng/mL). |