Comparison of Atypical /33-Adrenoceptor Agonists With Their Respective Metabolic Activities in Rat White Adipocytes

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Author(s)

Abstract

The metabolic activities of four types of β<SUB>3</SUB>-adrenoceptor (AR) agonists, BRL35135A, BRL28410, ICI215001 and CL316243, were compared with those of other β<SUB>1</SUB>- and β<SUB>2</SUB>-AR agonists in rat white adipocytes. All the β<SUB>3</SUB>-AR agonists caused cAMP formation, free fatty acid release and 2-deoxyglucose uptake; the maximum activity levels were similar except for ICI215001, which was lower. However, the magnitude of potency and selectivity of these agonists differed. The most potent and selective β<SUB>3</SUB>-agonist was CL316243. Metabolic activities and Northern blotting showed that there were three β-AR subtypes that were coupled to adenylyl cyclase and contributed to the induction of lipolysis and glucose uptake. The rank order of the amounts of β-AR subtypes was β<SUB>3</SUB>>>β<SUB>1</SUB> > β<SUB>2</SUB>. However, the physiological functions of β-AR subtypes were essentially similar in rat white adipocytes. On the other hand, cAMP accumulation and Northern blotting showed that human adipocytes predominantly contained β<SUB>2</SUB>-AR, with far lower levels of β<SUB>1</SUB>- and β<SUB>3</SUB>-ARs. These findings suggested that the β<SUB>3</SUB>-AR plays an important role in energy metabolism and thermogenesis in which cross talk exists between β<SUB>1</SUB>- and β<SUB>3</SUB>-ARs in rat adipocytes, while β<SUB>2</SUB>-AR is the most important for the lipolysis regulation in human subcutaneous adipocytes.

Journal

  • The Japanese Journal of Pharmacology

    The Japanese Journal of Pharmacology 77(1), 41-51, 1998-05-01

    The Japanese Pharmacological Society

References:  44

Codes

  • NII Article ID (NAID)
    10008680113
  • NII NACSIS-CAT ID (NCID)
    AA00691188
  • Text Lang
    ENG
  • Article Type
    ART
  • ISSN
    00215198
  • NDL Article ID
    4503673
  • NDL Source Classification
    ZS51(科学技術--薬学)
  • NDL Call No.
    Z53-D199
  • Data Source
    CJP  NDL  J-STAGE 
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