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Merck
CN

S7389

SB-269970 hydrochloride

powder, ≥98% (HPLC)

Synonym(s):

(R)-3-[2-[2-(4-Methylpiperidin-1-yl)ethyl]pyrrolidine-1-sulfonyl]phenol hydrochloride, SB 269970A

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About This Item

Empirical Formula (Hill Notation):
C18H28N2O3S · HCl
CAS Number:
261901-57-9
Molecular Weight:
388.95
NACRES:
NA.77
PubChem Substance ID:
24278708
UNSPSC Code:
12352200
MDL number:
MFCD03788020

Key Documents

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Product Name

SB-269970 hydrochloride, powder, ≥98% (HPLC)

InChI

1S/C18H28N2O3S.ClH/c1-15-7-11-19(12-8-15)13-9-16-4-3-10-20(16)24(22,23)18-6-2-5-17(21)14-18;/h2,5-6,14-16,21H,3-4,7-13H2,1H3;1H/t16-;/m1./s1

SMILES string

Cl.CC1CCN(CC1)CC[C@H]2CCCN2S(=O)(=O)c3cccc(O)c3

InChI key

XQCJOYZLWFNDIO-PKLMIRHRSA-N

assay

≥98% (HPLC)

form

powder

optical activity

[α]/D 75 to 90°, c = 1.0 in DMSO

storage condition

desiccated

solubility

H2O: 10 mg/mL, clear (warmed to 60 °C)

storage temp.

2-8°C

Quality Level

100

Gene Information

human ... HTR7(3363)

Biochem/physiol Actions

SB-269970 is an anti-psychotic agent that shows high affinity for 5-HT7 receptors. It may be effective in treating cognitive disabilities and schizophrenia-like deficits.4 SB-269970 desensitizes and decreases the excitatory effects of 5-HT7 receptors in rat hippocampus.5
Selective 5-HT7 serotonin receptor antagonist.

Legal Information

Sold with the permission of GlaxoSmithKline Pharmaceuticals

Application

SB-269970 hydrochloride has been used to study the effect of different endotype combination on the activity of the 5-hydroxytryptamine receptor of tall fescue alkaloids. It has also been used to inhibit dopamine receptor signaling, in order to study its role in early hemocyte activation.
SB-269970 was used to study the role of 5-HT7 receptors in serotonin-induced hypothermia in rodents.6

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)

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Certificates of Analysis (COA)

Lot/Batch Number
0000151460
0000151459
0000151459
0000151460
0000118107

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Krzysztof Tokarski et al.
Pharmacological reports : PR, 64(2), 256-265 (2012-06-05)
SB 269970, a 5-HT(7) receptor antagonist may produce a faster antidepressant-like effect in animal models, than do antidepressant drugs, e.g., imipramine. The present work was aimed at examining the effect of single and repeated (14 days) administration of SB 269970
J J Hagan et al.
British journal of pharmacology, 130(3), 539-548 (2000-05-24)
The novel 5-HT(7) receptor antagonist, SB-269970-A, potently displaced [(3)H]-5-CT from human 5-HT(7(a)) (pK(i) 8.9+/-0.1) and 5-HT(7) receptors in guinea-pig cortex (pK(i) 8.3+/-0.2). 5-CT stimulated adenylyl cyclase activity in 5-HT(7(a))/HEK293 membranes (pEC(50) 7.5+/-0.1) and SB-269970-A (0.03 - 1 microM) inhibited the
Peter B Hedlund et al.
European journal of pharmacology, 487(1-3), 125-132 (2004-03-23)
Studies using selective drugs and knockout mice have demonstrated that the 5-HT(7) receptor plays an instrumental role in serotonin-induced hypothermia. There is also evidence supporting an involvement of the 5-HT(1A) receptor, although mainly from studies using 8-hydroxy-2(di-n-propylamino)tetralin (8-OH-DPAT), a 5-HT(1A/7)
A novel, potent, and selective 5-HT(7) antagonist: (R)-3-(2-(2-(4-methylpiperidin-1-yl)ethyl)pyrrolidine-1-sulfonyl) phen ol (SB-269970).
P J Lovell et al.
Journal of medicinal chemistry, 43(3), 342-345 (2000-02-12)
Ilknur Calik et al.
Inflammopharmacology, 28(4), 893-902 (2020-06-07)
This study aimed to demonstrate the role of serotonin 7 receptor (5-HT7) and the effects of 5-HT7 agonists and antagonists in an indomethacin-induced gastric ulcer. Male albino Wistar rats (n = 60) were used in the experiments. LP44 (5-HT7 agonist) and SB269970 (5-HT7
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