A-331440 dihydrochloride

• Catalog No.: A7730
• CAS Number: 392338-13-5(freebase)
• M. F.: C22H29Cl2N3O
• M. W.: 422.39116
• Purity: ≥98% (HPLC)
• Storage: desiccated

SYNONYMS

• IUPAC name: 4-(4-{3-[(3R)-3-(dimethylamino)pyrrolidin-1-yl]propoxy}phenyl)benzonitrile dihydrochloride
• IUPAC Traditional name: 4-(4-{3-[(3R)-3-(dimethylamino)pyrrolidin-1-yl]propoxy}phenyl)benzonitrile dihydrochloride
• Synonyms: 4’-[3-[(3(R)-Dimethylamino-1-pyrrolidinyl]propoxy]-[1,1-biphenyl]-4‘-carbonitrile dihydrochloride

DATABASE IDS

• CAS Number: 392338-13-5(freebase)
• PubChem SID: 24724398

PROPERTIES

• Empirical Formula (Hill Notation): C22H27N3O · 2HCl
• Purity: ≥98% (HPLC)
• Apperance: white to off-white solid
• Solubility: H2O: ≥10 mg/mL
• GHS Signal Word: Warning
• GHS Hazard statements: H319
• Personal Protective Equipment: Eyeshields, Gloves, type N95 (US), type P1 (EN143) respirator filter
• GHS Precautionary statements: P305 + P351 + P338
• Storage Condition: desiccated
• Storage Temperature: 2-8°C
• German water hazard class: 3

DETAILS

Description (English)

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.

Description (简体中文)

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.