Batra S, Biörklund A
Psychopharmacology (Berl). 1986;90(1):1-4. doi: 10.1007/BF00172861.
The binding kinetics of tritiated quinuclidinyl benzilate (QNB) were studied in membrane preparations from human parotid and rabbit submandibular glands. Inhibition of 3H-QNB was then used to compare the anticholinergic activity of lofepramine, desipramine, imipramine and amitriptyline for muscarinic receptor in the salivary glands. The apparent dissociation constant (KD) for 3H-QNB binding in human parotid and rabbit submandibular gland was 33 and 61 pM and the Bmax value 507 and 169 f mol/mg protein, respectively. The mean values for the inhibition constant (Ki) for lofepramine, desipramine, imipramine and amitriptyline in human parotid gland were 285, 135, 102 and 13 nM, respectively. Very similar values were obtained for the rabbit submandibular gland. The binding affinity of tricyclic antidepressants for muscarinic cholinergic receptor sites in human parotid gland closely paralleled clinical data on the inhibition of salivary flow by these drugs.
在人腮腺和兔下颌下腺的膜制剂中研究了氚化苄哌苯胺（QNB）的结合动力学。然后利用3H-QNB抑制作用比较了洛非帕明、地昔帕明、丙咪嗪和阿米替林对唾液腺毒蕈碱受体的抗胆碱能活性。人腮腺和兔下颌下腺中3H-QNB结合的表观解离常数（KD）分别为33和61 pM，Bmax值分别为507和169 fmol/mg蛋白。洛非帕明、地昔帕明、丙咪嗪和阿米替林在人腮腺中的抑制常数（Ki）平均值分别为285、135、102和13 nM。兔下颌下腺也得到了非常相似的值。三环类抗抑郁药对人腮腺毒蕈碱胆碱能受体位点的结合亲和力与这些药物抑制唾液分泌的临床数据密切相关。
