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激动剂和拮抗剂与猪脂肪组织β-肾上腺素能受体的结合

Binding of agonists and antagonists to the porcine adipose tissue beta-adrenergic receptor(s).

作者信息

Mersmann H J, Akanbi K, Shparber A, McNeel R L

机构信息

USDA/ARS Children's Nutrition Research Center, Department of Pediatrics, Baylor College of Medicine, Houston, TX 77030.

出版信息

Comp Biochem Physiol C Comp Pharmacol Toxicol. 1993 Nov;106(3):725-32. doi: 10.1016/0742-8413(93)90233-b.

Abstract
  1. Affinities of agonists for porcine adipose tissue beta-adrenergic receptors, determined by competitive ligand binding with 3H-dihydroalprenolol to crude adipose tissue membranes in vitro, varied from 50 times > to 25 times < than isoproterenol. Affinities for antagonists varied from 8 times > to 1000 times < propranolol. 2. Receptor affinity was not related to the ability to stimulate or inhibit lipolysis, or to the agonist or antagonist purported receptor subtype specificity. 3. Modeling of ligand-binding data indicated more than one binding site for several ligands. The assignment of beta-adrenergic subtypes to the individual binding sites was unclear because this would depend on the individual ligands used to establish binding sites.
摘要
  1. 通过在体外将激动剂与³H-二氢阿普洛尔竞争性结合于粗制脂肪组织膜来测定激动剂对猪脂肪组织β-肾上腺素能受体的亲和力,其变化范围比异丙肾上腺素高50倍至低25倍。拮抗剂的亲和力变化范围比普萘洛尔高8倍至低1000倍。2. 受体亲和力与刺激或抑制脂肪分解的能力无关,也与所谓的激动剂或拮抗剂受体亚型特异性无关。3. 配体结合数据建模表明几种配体存在不止一个结合位点。由于这取决于用于确定结合位点的个别配体,因此不清楚各个结合位点对应的β-肾上腺素能亚型。

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