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Merck

A7730

Sigma-Aldrich

A-331440 dihydrochloride

≥98% (HPLC), solid

Sinónimos:

4’-[3-[(3(R)-Dimethylamino-1-pyrrolidinyl]propoxy]-[1,1-biphenyl]-4‘-carbonitrile dihydrochloride

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About This Item

Fórmula empírica (notación de Hill):
C22H27N3O · 2HCl
Número de CAS:
Peso molecular:
422.39
MDL number:
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77

Quality Level

assay

≥98% (HPLC)

form

solid

storage condition

desiccated

color

white to off-white

solubility

H2O: ≥10 mg/mL

originator

Abbott

storage temp.

2-8°C

SMILES string

CN([C@H]1CN(CCCOC2=CC=C(C3=CC=C(C#N)C=C3)C=C2)CC1)C.[H]Cl.[H]Cl

InChI

1S/C22H27N3O.2ClH/c1-24(2)21-12-14-25(17-21)13-3-15-26-22-10-8-20(9-11-22)19-6-4-18(16-23)5-7-19;;/h4-11,21H,3,12-15,17H2,1-2H3;2*1H/t21-;;/m1../s1

InChI key

XFPYVTSGYYMTFS-GHVWMZMZSA-N

Biochem/physiol Actions

A-331440 dihydrochloride is a non-imidazole H3 histamine receptor antagonist. Presynaptic histamine H(3) receptors regulate release of histamine and other neurotransmitters, and histamine H(3) receptor antagonists enhance neurotransmitter release. A-331440 is a histamine H(3) receptor antagonist, which binds potently and selectively to both human and rat histamine H(3) receptors (K(i)=25 nM). Mice on a high-fat diet (45 kcal % lard) prior to 28-day oral b.i.d. dosing for measurement of obesity-related parameters. A-331440 administered at 0.5 mg/kg had no significant effect on weight, whereas 5 mg/kg decreased weight comparably to dexfenfluramine (10 mg/kg). A-331440 administered at 15 mg/kg reduced weight to a level comparable to mice on the low-fat diet. The two higher doses reduced body fat and the highest dose also normalized an insulin tolerance test. Both data shows that the histamine H(3) receptor antagonist, A-331440, has potential as an antiobesity agent.

Features and Benefits

This compound is featured on the Histamine Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
This compound was developed by Abbott. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)


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