Carlsson E, Dahlöf C G, Hedberg A, Persson H, Tångstrand B
Naunyn Schmiedebergs Arch Pharmacol. 1977 Nov;300(2):101-5. doi: 10.1007/BF00505039.
The relative inotropic and chronotropic activity of beta-adrenoceptor agonists was studied in the noradrenaline-depleted, anaesthetized cat. Terbutaline, a selective beta2-adrenoceptor agonist, gave at a certain dose a more pronounced chronotropic than inotropic response, while a new beta1-selective adrenoceptor agonist (-)-H 80/62 produced the same degree of chronotropic and inotropic stimulation. The results indicate that there is some difference between the beta-adrenoceptors in the sinus node mediating chronotropic stimulation and beta-adrenoceptors in the ventricular myocardium mediating stimulation of the contractile force. It has been shown that there are both beta1- and beta2-adrenoceptors in the heart (Carlsson et al., 1972). In the light of this finding it is hypothetized that there are differences in the relative distribution of beta1- and beta2-adrenoceptors in the sinus node and in the myocardium. Athough beta1 is the predominant type of beta-adrenoceptor in both regions, the beta1:beta2 concentration ratio seems to be higher in the myocardium, than in the sinus node.
在去甲肾上腺素耗竭的麻醉猫身上研究了β-肾上腺素能受体激动剂的相对变力性和变时性活性。特布他林是一种选择性β2-肾上腺素能受体激动剂,在一定剂量下产生的变时性反应比变力性反应更明显,而一种新的β1-选择性肾上腺素能受体激动剂(-)-H 80/62产生的变时性和变力性刺激程度相同。结果表明,介导变时性刺激的窦房结中的β-肾上腺素能受体与介导收缩力刺激的心室心肌中的β-肾上腺素能受体之间存在一些差异。已表明心脏中存在β1-和β2-肾上腺素能受体(卡尔森等人,1972年)。鉴于这一发现,推测β1-和β2-肾上腺素能受体在窦房结和心肌中的相对分布存在差异。虽然β1是这两个区域中主要的β-肾上腺素能受体类型,但β1:β2浓度比在心肌中似乎高于窦房结。