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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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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)

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

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

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
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)
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
Agnieszka Nikiforuk et al.
PloS one, 8(6), e66695-e66695 (2013-06-19)
A wide body of evidence suggests that 5-HT7 receptors are implicated in a variety of central nervous system functions, including control of learning and memory processes. According to recent preclinical data, the selective blockade of these receptors may be a
D R Thomas et al.
British journal of pharmacology, 130(2), 409-417 (2000-05-12)
Binding of the 5-HT(7) receptor antagonist radioligand [(3)H]-SB-269970 to human 5-HT(7(a)) receptors expressed in HEK293 cell membranes (h5-HT(7(a))/293) and to guinea-pig cerebral cortex membranes, was characterized and compared with [(3)H]-5-CT binding. [(3)H]-SB-269970 (1 nM) showed full association with h5-HT(7(a))/293 membranes
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