A7730

A-331440 dihydrochloride

≥98% (HPLC), solid

• Synonyme(s) : 4’-[3-[(3(R)-Dimethylamino-1-pyrrolidinyl]propoxy]-[1,1-biphenyl]-4‘-carbonitrile dihydrochloride
• Formule empirique (notation de Hill): C₂₂H₂₇N₃O · 2HCl
• Numéro CAS: 392338-13-5
• Poids moléculaire : 422.39
• Numéro MDL: MFCD08705336
• Code UNSPSC : 12352200
• ID de substance PubChem : 24724398
• Nomenclature NACRES : NA.77

Propriétés

• Pureté: ≥98% (HPLC)
• Forme: solid
• Conditions de stockage: desiccated
• Couleur: white to off-white
• Solubilité: H₂O: ≥10 mg/mL
• Auteur: Abbott
• Température de stockage: 2-8°C
• Chaîne SMILES: 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
• Clé InChI: XFPYVTSGYYMTFS-GHVWMZMZSA-N

Description

Actions biochimiques/physiologiques

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.

Caractéristiques et avantages

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.

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable
• Équipement de protection individuelle: Eyeshields, Gloves, type N95 (US)