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文件

S3313

SB-204070 盐酸盐

Name: SB-204070 盐酸盐
Brand: SIGMA

solid, ≥97% (HPLC)

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别名:

（1-丁基-4-哌啶基）甲基-8-氨基-7-氯-1,4-苯并二恶烷-5-羧酸盐盐酸盐

经验公式（希尔记法）:

C₁₉H₂₇ClN₂O₄ · HCl

CAS号:

148702-58-3

分子量:

419.34

MDL编号:

MFCD03453014

PubChem化学物质编号:

24278704

NACRES:

NA.77

质量水平

100

检测方案

≥97% (HPLC)

形式

solid

mp

243-245 °C (lit.)

溶解性

H₂O: 20 mg/mL (with heating)

SMILES字符串

Cl[H].CCCCN1CCC(CC1)COC(=O)c2cc(Cl)c(N)c3OCCOc23

InChI

1S/C19H27ClN2O4.ClH/c1-2-3-6-22-7-4-13(5-8-22)12-26-19(23)14-11-15(20)16(21)18-17(14)24-9-10-25-18;/h11,13H,2-10,12,21H2,1H3;1H

InChI key

YEQGKAOSYSXEPU-UHFFFAOYSA-N

基因信息

human ... HTR4(3360)

应用

SB-204070盐酸盐用于研究5-HT代谢产物在胰蛋白酶诱导的小鼠盲肠阴离子分泌中的作用。

生化/生理作用

SB-204070是4-HT₄受体的高效特异性拮抗剂。它抑制胆碱能和非胆碱能传递，并阻断豚鼠近端结肠的收缩和人结肠环状平滑肌的松弛。

选择性5-HT₄ 血清素受体拮抗剂。

法律信息

在葛兰素史克制药公司的独家许可下生产和销售

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

个人防护装备

Eyeshields, Gloves, type N95 (US)

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Evidence for 5-HT7 receptors mediating relaxation of human colonic circular smooth muscle.

N H Prins et al.

British journal of pharmacology, 128(4), 849-852 (1999-11-11)

5-HT4 receptors mediate relaxation of human colon circular muscle. However, after 5-HT4 receptor blockade (SB 204070 10 nM), 5-HT still induced a relaxation (pEC50 6.3). 5-HT4 receptors were sufficiently blocked, as the curves to 5-HT obtained in the presence of

Peripheral 5-HT4 receptors.

S S Hegde et al.

FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 10(12), 1398-1407 (1996-10-01)

The 5-HT4 receptor is a member of the seven transmembrane spanning G-protein-coupled family of receptors. The receptor is positively coupled to adenylate cyclase and exists in two isoforms (5-HT4S and 5-HT4L) that differ in the length and sequence of their

Pharmacological characterization of the human 5-HT(4(d)) receptor splice variant stably expressed in Chinese hamster ovary cells.

J Mialet et al.

British journal of pharmacology, 131(4), 827-835 (2000-10-13)

The recently identified C-terminal splice variant of the human 5-HT(4) receptor, the h5-HT(4(d)) receptor, was stably expressed in a CHO cell line at 493+/-25 fmol mg(-1) protein. We analysed its pharmacological properties by measuring binding affinities and 5-HT(4) ligand-induced cyclic

The effects of SB 204070, a highly potent and selective 5-HT4 receptor antagonist, on guinea-pig distal colon.

K A Wardle et al.

British journal of pharmacology, 112(3), 789-794 (1994-07-01)

1. The pharmacology of a novel 5-HT4 receptor antagonist, SB 204070 has been evaluated in the guinea-pig isolated distal colon longitudinal muscle-myenteric plexus (LMMP). 2. SB 204070 is a highly potent antagonist of 5-HT-evoked cholinergically-mediated contractions in the guinea-pig distal

(1-Butyl-4-piperidinyl)methyl 8-amino-7-chloro-1,4-benzodioxane-5-carboxylate hydrochloride: a highly potent and selective 5-HT4 receptor antagonist derived from metoclopramide.

L M Gaster et al.

Journal of medicinal chemistry, 36(25), 4121-4123 (1993-12-10)

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