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SB 699551 dihydrochloride

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Chemical Structure| 864741-95-7 同义名 : SB-699551
CAS号 : 864741-95-7
货号 : A822692
分子式 : C34H47Cl2N3O
纯度 : 98%
分子量 : 584.663
MDL号 : MFCD11112202
存储条件:

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 120 mg/mL(205.25 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 SB-699551 is a 5-HT5A receptor antagonist. SB-699551 (0.1 mg/kg) decreased lever-press conditioned responses (CR) during short-term (STM; 1.5-h) or (3.0 mg/kg) long-term memory (LTM; 24-h); relative to the vehicle animals. SB-699551 (0.3 mg/kg) alone also produced amnesia-like effect[1]. SB-699551-A showed an anxiolytic-like property in the ultrasonic vocalization test[2]. SB-699551 has efficiency in ameliorating ketamine-induced impairments on the ASST (attentional set-shifting task) and NORT (ovel object recognition task)[3]. SB-699551 ((1-10mg/kg, i.p.) nor SB-269970 (5-HT(7) antagonist, 1-10mg/kg, i.p.) reduced the 5-HTP (5-hydroxytryptophan) and HAL(haloperidol)-induced bradykinesia or catalepsy[4]. SB-699551 significantly reduced the antinociceptive effect of both WIN 55,212-2 and morphine[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.71mL

0.34mL

0.17mL

8.55mL

1.71mL

0.86mL

17.10mL

3.42mL

1.71mL

参考文献

[1]Aparicio-Nava L, Márquez-García LA, Meneses A. Effects of 5-HT5A receptor blockade on amnesia or forgetting. Behav Brain Res. 2019 Jan 14;357-358:98-103

[2]Kassai F, Schlumberger C, Kedves R, Pietraszek M, Jatzke C, Lendvai B, Gyertyán I, Danysz W. Effect of 5-HT5A antagonists in animal models of schizophrenia, anxiety and depression. Behav Pharmacol. 2012 Aug;23(4):397-406

[3]Nikiforuk A, Hołuj M, Kos T, Popik P. The effects of a 5-HT5A receptor antagonist in a ketamine-based rat model of cognitive dysfunction and the negative symptoms of schizophrenia. Neuropharmacology. 2016 Jun;105:351-360

[4]Ohno Y, Imaki J, Mae Y, Takahashi T, Tatara A. Serotonergic modulation of extrapyramidal motor disorders in mice and rats: role of striatal 5-HT3 and 5-HT6 receptors. Neuropharmacology. 2011 Feb-Mar;60(2-3):201-8

[5]Aksu AG, Gunduz O, Ulugol A. Contribution of spinal 5-HT5A receptors to the antinociceptive effects of systemically administered cannabinoid agonist WIN 55,212-2 and morphine. Can J Physiol Pharmacol. 2018 Jun;96(6):618-623