Neuropeptide S human 是有效的内源性 neuropeptide S receptor 激动剂 (EC50=9.4 nM)。Neuropeptide S human (TFA) 可提高小鼠的运动活性和清醒性。Neuropeptide S human 有潜力用于阿尔茨海默症 (AD) 的研究。
Neuropeptide S human (4 pM to 1.7 nM; 48 hours) retains full agonist activity with an EC
50
of 6.7 ± 2.4 nM, the binding of [
125I
] Y10-hNPS to CHO cells stably expressing hNPSR is saturable with high affinity (K
d
= 0.33 ± 0.12 nM).
Neuropeptide S human (1 pM-3 μM; 48 hours) are used to compete with 0.15 nM [
125I
I] Y10-NPS, [
125I
I] Y10-NPS is displaceable by increasing concentrations of human NPS (IC
50
= 0.42 ± 0.12 nM).
Neuropeptide S human (0.1 nM-1 nM; i.c.v.) causes a significant increase in locomotor activity, the total distance traveled, percentage of time moving, number of rearing events, and center entries are also significantly increased in mice.
Animal Model:
Male C57Bl/6 mice
Dosage:
0.1 nM, 1 nM
Administration:
Intracerebroventricular (i.c.v.) injection
Result:
Increased locomotor activity and promoted wakefulness.
