Raasmaja A, Mohell N, Nedergaard J
Eur J Pharmacol. 1984 Nov 27;106(3):489-98. doi: 10.1016/0014-2999(84)90052-9.
Binding sites for [3H]prazosin were characterized in crude membrane fractions from rat brown adipose tissue. Based on agonist (norepinephrine approximately equal to phenylephrine much greater than isoprenaline) and antagonist (prazosin much greater than yohimbine greater than propranolol) potencies to compete with [3H]prazosin, the binding sites were identified as alpha 1-receptors, not previously described in rat brown adipose tissue. As the [3H]prazosin binding sites could be observed in isolated brown fat cell preparations, they were probably postsynaptic. The effect of cold acclimation was studied in crude membrane fractions from control and cold-acclimated (4 degrees C) rats and hamsters. Cold acclimation did not change the affinity of the receptor for agonists and antagonists, but there was a significant increase in the number of alpha 1-receptors (per mg protein), both in rat (100% increase) and hamster (40% increase) brown fat. Based on these results and on earlier results on beta-receptors from this and other laboratories, it is suggested that activation of brown adipose tissue is associated with an increase in the relative density of alpha 1-receptors (i.e. in the alpha 1/beta ratio) and an increased significance of alpha 1-adrenergic pathways for the function of the tissue.
利用大鼠棕色脂肪组织的粗制膜组分对[³H]哌唑嗪的结合位点进行了特性研究。根据激动剂(去甲肾上腺素≈苯肾上腺素>>异丙肾上腺素)和拮抗剂(哌唑嗪>>育亨宾>普萘洛尔)与[³H]哌唑嗪竞争的效力,确定这些结合位点为α₁受体,此前在大鼠棕色脂肪组织中未曾描述过。由于在分离的棕色脂肪细胞制剂中可观察到[³H]哌唑嗪结合位点,它们可能位于突触后。研究了对照大鼠和冷适应(4℃)大鼠及仓鼠的粗制膜组分中冷适应的影响。冷适应并未改变受体对激动剂和拮抗剂的亲和力,但大鼠(增加100%)和仓鼠(增加40%)棕色脂肪中α₁受体的数量(每毫克蛋白质)均显著增加。基于这些结果以及本实验室和其他实验室关于β受体的早期结果,提示棕色脂肪组织的激活与α₁受体相对密度的增加(即α₁/β比值增加)以及α₁肾上腺素能途径对该组织功能的重要性增加有关。