S3313

Sigma-Aldrich

SB-204070 hydrochloride

solid, ≥97% (HPLC)

Synonym(s):
(1-Butyl-4-piperidinyl)methyl-8-amino-7-chloro-1,4-benzodioxane-5-carboxylate hydrochloride
Empirical Formula (Hill Notation):
C19H27ClN2O4 · HCl
CAS Number:
Molecular Weight:
419.34
MDL number:
PubChem Substance ID:
NACRES:
NA.77
Pricing and availability is not currently available.

assay

≥97% (HPLC)

form

solid

mp

243-245 °C (lit.)

solubility

H2O: 20 mg/mL (with heating)

SMILES string

ClH.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

Gene Information

human ... HTR4(3360)

Application

SB-204070 hydrochloride was used to study the role of 5-HT metabolites in trypsin-induced anion secretion in mouse cecum.

Packaging

5, 25 mg in glass bottle

Biochem/physiol Actions

SB-204070 is a highly potent and specific antagonist of 4-HT4 receptor. It inhibits cholinergic and noncholinergic transmission and blocks the contractions of proximal colon in guinea pigs and relaxation of human colon circular smooth muscle.
Selective 5-HT4 serotonin receptor antagonist.

Legal Information

Manufactured and sold under exclusive license from GlaxoSmithKline Pharmaceuticals

Personal Protective Equipment

dust mask type N95 (US),Eyeshields,Gloves

RIDADR

NONH for all modes of transport

WGK Germany

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificate of Analysis
Certificate of Origin
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)
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...
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...
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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