RS 67506 hydrochloride
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
pKi:8.8
RS 67506 hydrochloride是一种强效的和选择性的5-HT4部分激动剂。
5-HT4受体的选择性激动剂不仅可以增强认知功能,促进肠胃蠕动,还可以纠正与逼尿肌运动减弱有关的排尿紊乱,或作为止痛药。
体外:对调节卡巴胆碱预收缩食管松弛的5-HT4受体上的5-HT而言,RS 67506是一种强效的部分激动剂。对RS 67506的舒张反应被可克服性拮抗,表观亲和力(pKB)为9.0。因此,RS 67506在体外作为强效的5-HT4受体部分激动剂。凭借高效力和选择性,该化合物可用于阐明5-HT4受体的生理作用 [1]。
体内:RS 67506诱导麻醉微小型猪心率剂量依赖性的增强(ED50 5.4 pg kg-1, i.v.) ,最大增加47 beats min-1 [1]。此外,在空间学习和记忆大鼠模型中,研究了两种新的强效的和选择性的5-HT4受体激动剂(RS67333和RS67506)的作用。相比之下,未发现RS67506 (0.1、10 和1000 pg/kg, i.p.)与RS67333等效的效力和选择性。这一不同结果可能表明RS67333相对于RS67506进入CNS的能力增强[2]。
临床试验:目前尚未进行临床研究。
参考文献:
[1]. Eglen RM, Bonhaus DW, Johnson LG, Leung E, Clark RD. Pharmacological characterization of two novel and potent 5-HT4 receptor agonists, RS 67333 and RS 67506, in vitro and in vivo. Br J Pharmacol. 1995 Aug;115(8):1387-92.
[2]. Fontana DJ, Daniels SE, Wong EH, Clark RD, Eglen RM. The effects of novel, selective 5-hydroxytryptamine (5-HT) 4 receptor ligands in rat spatial navigation. Neuropharmacology. 1997 Apr-May;36(4-5):689-96.
Storage | Store at RT |
M.Wt | 454.41 |
Cas No. | 168986-61-6 |
Formula | C18H28ClN3O4S·HCl |
Solubility | Soluble to 80 mM in H2O |
Chemical Name | N-(2-(4-(3-(4-amino-5-chloro-2-methoxyphenyl)-3-oxopropyl)piperidin-1-yl)ethyl)methanesulfonamide hydrochloride |
SDF | Download SDF |
Canonical SMILES | ClC(C=C(C(OC)=C1)C(CCC2CCN(CCNS(=O)(C)=O)CC2)=O)=C1N.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
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