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Merck
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重要文件

S3313

Sigma-Aldrich

SB-204070 盐酸盐

solid, ≥97% (HPLC)

同義詞:

(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

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About This Item

經驗公式(希爾表示法):
C19H27ClN2O4 · HCl
CAS號碼:
分子量::
419.34
MDL號碼:
分類程式碼代碼:
12352200
PubChem物質ID:
NACRES:
NA.77

品質等級

化驗

≥97% (HPLC)

形狀

solid

mp

243-245 °C (lit.)

溶解度

H2O: 20 mg/mL (with heating)

SMILES 字串

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 密鑰

YEQGKAOSYSXEPU-UHFFFAOYSA-N

基因資訊

human ... HTR4(3360)

應用

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。

法律資訊

在葛兰素史克制药公司的独家许可下生产和销售

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable

個人防護裝備

Eyeshields, Gloves, type N95 (US)


分析證明 (COA)

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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
(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)
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
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
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

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