Respective degree of expression of beta 1-, beta 2- and beta 3-adrenoceptors in human brown and white adipose tissues

• Published in: British journal of pharmacology Vol. 118; no. 4; pp. 929 - 934
• Main Authors: Deng, C, Paoloni-Giacobino, A, Kuehne, F, Boss, O, Revelli, J P, Moinat, M, Cawthorne, M A, Muzzin, P, Giacobino, J P
• Format: Journal Article
• Language: English
• Published: England 01.06.1996
• Subjects: Adipose Tissue - metabolism; Adipose Tissue, Brown - metabolism; Adrenergic beta-Agonists - metabolism; Adrenergic beta-Antagonists - metabolism; Adult; Aged; Binding Sites; Ethanolamines - metabolism; Female; Humans; Male; Middle Aged; Propanolamines - metabolism; Receptors, Adrenergic, beta - genetics; Receptors, Adrenergic, beta - metabolism; Receptors, Adrenergic, beta-1 - genetics; Receptors, Adrenergic, beta-1 - metabolism; Receptors, Adrenergic, beta-2 - genetics; Receptors, Adrenergic, beta-2 - metabolism; Receptors, Adrenergic, beta-3; RNA, Messenger - genetics; RNA, Messenger - metabolism; Stereoisomerism
• ISSN: 0007-1188; 1476-5381
• DOI: 10.1111/j.1476-5381.1996.tb15488.x

1. The possible existence of a beta 3-adrenoceptor in human brown and white adipose tissues was investigated by mRNA expression and binding studies. 2. The relative amounts of beta 1-, beta 2- and beta 3-adrenoceptor mRNA, as determined by total RNA Northern blot analysis in newborn brown adipose tissue, were 28, 63 and 9% respectively of the total beta-adrenoceptor mRNA. 3. The beta 1/beta 2-adrenoceptors of human brown adipose tissue plasma membranes were characterized using [3H]-CGP 12177 as a ligand. Their Kd and Bmax values were 1.9 nM and 156 fmol mg-1 of membrane proteins, respectively. The beta 3-adrenoceptor was characterized by use of the new specific radioligand [3H]-SB 206606. The binding of this ligand was stereospecifically displaced by the active R,R- or the inactive S,S-enantiomer of BRL 37344 up to a concentration of about 10 microM. The Kd and Bmax values of the brown adipose tissue membrane beta 3-adrenoceptors were 87 nM and 167 fmol mg-1 of proteins, respectively. A low affinity [3H]-CGP 12177 binding site population was also detected in these membranes. 4. In human omental white adipose tissue, no beta 3-adrenoceptor mRNA could be detected in total RNA Northern blots and the beta 1-and beta 2-adrenoceptor mRNAs represented 9 and 91%, respectively of the total beta-adrenoceptor mRNA, and no specific binding of [3H]-SB 206606 could be measured.