Anti-Obesity Effects of Selective Agonists to the .BETA.3-Adrenergic Receptor in Dogs. I. The Presence of Canine .BETA.3-Adrenergic Receptor and in vivo Lipomobilization by Its Agonists.

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  • SASAKI Noriyasu
    Laboratory of Biochemistry, Department of Biomedical Sciences, School of Veterinary Medicine, Hokkaido University
  • UCHIDA Eiji
    Department of Internal Medicine II, Rakuno Gakuen University
  • NIIYAMA Masayoshi
    Department of Internal Medicine II, Rakuno Gakuen University
  • YOSHIDA Toshihide
    Department of Internal Medicine, Kyoto Prefectural University of Medicine
  • SAITO Masayuki
    Laboratory of Biochemistry, Department of Biomedical Sciences, School of Veterinary Medicine, Hokkaido University

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  • Anti-obesity effects of selective agonists to the β3-adrenergic receptor in dogs(1)The presence of canine β3-adrenergic receptor and in vivo lipomobilization by its agonists
  • Anti-obesity effects of selective agoni

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Abstract

It is known that in rodents and humans the β3-adrenergic receptor (β3-AR) is present primarily in adipocytes and plays a significant role in the adrenergic stimulation of lipolysis. We examined the expression of β3-AR mRNA in the dog and the lipomobilizing effects of β3-AR-selective agonists in vivo. Reverse transcription polymerase chain reaction of RNA extracted from dog adipose tissue produced a cDNA fragment, the nucleotide sequence of which was highly homologous to the corresponding regions of human (86.4%) and mouse (79.5%) β3-AR cDNA. The β3-AR mRNA was present at high levels in subcutaneous and visceral adipose tissues, but undetectable in other organs. When a selective β3-AR agonist, CL316, 243, was infused intravenously into beagle dogs, the plasma level of free fatty acid increased in 30 min and persisted at higher levels for several hours. ICI D7114, another β3-AR agonist, also showed a similar lipomobilizing effect, but with lower potency. β3-AR agonist infusion also increased the plasma insulin level. These results suggested that functional β3-AR is present in adipose tissues of the dog and that it is effective for in vivo lipomobilization.

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