SB-334867 free base |
| Catalog No.GC15034 |
SB-334867 유리염기(SB334867A 유리염기)는 우수한 선택적 혈액뇌장벽 투과성 오렉신-1(OX1) 수용체 길항제로, OX2(pKb=7.4)에 대해 선택성을 나타내며, 5-HT2B에 대해 100배, 5- pKi 값이 각각 5.4 및 5.3인 HT2C.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 792173-99-0
Sample solution is provided at 25 µL, 10mM.
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SB-334867 free base is a selective antagonist of orexin-1 receptor [1].
Orexin-A and orexin-B are two peptides isolated from rat hypothalamus. They are involved in some physiological functions such as the control of feeding, energy metabolism and regulation of the sleep-wake cycle.
SB-334867 free base could inhibit the orexin-A and orexin-B induced calcium responses in CHO-OX1 cells with pKB values of 7.27 and 7.23, respectively. SB-334867 was more selective for OX1 receptor over OX2 receptor. It caused 32.7% and 22% inhibition of orexin-A and orexin-B induced calcium responses in CHO-OX2 cells, respectively. Moreover, SB-334867 was found to reduce both orexin-A-induced and fasting-induced food intake. The acute anorectic effect of it was associated with significant reductions in all active behaviours [1, 2].
References:
[1] Smart D, Sabido-David C, Brough S J, et al. SB-334867-A: the first selective orexin-1 receptor antagonist. British journal of pharmacology, 2001, 132(6): 1179-1182.
[2] Rodgers R J, Halford J C G, Nunes de Souza R L, et al. SB-334867, a selective orexin-1 receptor antagonist, enhances behavioural satiety and blocks the hyperphagic effect of orexin-A in rats. European Journal of Neuroscience, 2001, 13(7): 1444-1452.
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