Beta-adrenergic receptor subtypes mediating lipolysis in porcine adipocytes. Studies with BRL-37344, a putative β3-adrenergic agonist

Comparative Biochemistry and Physiology Part C: Pharmacology, Toxicology and Endocrinology Pub Date : 2000-05-01 DOI:10.1016/S0742-8413(00)00086-4

Scott Mills

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引用次数: 12

Abstract

The β₃-selective adrenergic receptor ligand BRL 37344 (BRL) was used to differentiate the presence and functional role of β-adrenergic receptor (βAR) subtypes in pig tissues. BRL did not stimulate adenylyl cyclase in membrane preparations or increase lipolysis from pig adipocytes. In contrast to some species, BRL appears to be a poor agonist for the pig βAR and is not a useful β₃AR ligand. Based on displacement of [³H]dihydroalprenolol binding, BRL exhibited a 100-fold selectivity for pig βAR subtypes in adipose and skeletal muscle membranes. The high affinity site was proposed to be the β₂AR. When used as an antagonist, BRL blockade of the high affinity site did not interfere with isoproterenol-stimulated lipolysis but did inhibit adenylyl cyclase activation. Results indicate that the high affinity βAR (β₂AR) is not linked to lipolysis, possibly due to intracellular compartmentalization. Therefore, βAR subtypes may have function-specific effects.

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β -肾上腺素能受体亚型介导猪脂肪细胞的脂肪分解。β3-肾上腺素能激动剂BRL-37344的研究

利用β3选择性肾上腺素能受体配体BRL 37344 (BRL)来区分β-肾上腺素能受体(βAR)亚型在猪组织中的存在及其功能作用。BRL不会刺激膜制剂中的腺苷酸环化酶，也不会增加猪脂肪细胞的脂肪分解。与某些物种相比，BRL对猪β3AR似乎是一种较差的激动剂，并不是一种有用的β3AR配体。基于[3H]二氢阿普萘洛尔结合的位移，BRL在脂肪和骨骼肌膜中对猪βAR亚型具有100倍的选择性。高亲和力位点被认为是β2AR。当用作拮抗剂时，BRL阻断高亲和力位点不会干扰异丙肾上腺素刺激的脂肪分解，但会抑制腺苷酸环化酶的激活。结果表明，高亲和力βAR (β2AR)与脂肪分解无关，可能是由于细胞内区隔化。因此，βAR亚型可能具有功能特异性作用。

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Comparative Biochemistry and Physiology Part C: Pharmacology, Toxicology and Endocrinology

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