Richards M H
Marion Merrell Dow Research Institute, Strasbourg, France.
Eur J Pharmacol. 1991 Apr 3;195(3):403-5. doi: 10.1016/0014-2999(91)90483-7.
The affinities of cyproheptadine, pizotifen and (+/-)-quinuclidinyl xanthane-9-carboxylate hemioxylate (QNX) were determined at muscarinic autoreceptors and postsynaptic (IP1 formation) receptors in rat hippocampal slices. The affinity values for QNX were 8.2 and 8.5 respectively. Cyproheptadine and pizotifen were less potent than QNX. Pizotifen was slightly (2-fold) less active at antagonizing IP1 formation than blocking the autoreceptors whereas cyproheptadine was equally active at antagonizing the two hippocampal muscarinic receptors.
在大鼠海马切片的毒蕈碱自身受体和突触后(肌醇磷酸酯1形成)受体上测定了赛庚啶、苯噻啶和(±)-奎宁环基呫吨-9-羧酸半草酸盐(QNX)的亲和力。QNX的亲和力值分别为8.2和8.5。赛庚啶和苯噻啶的效力低于QNX。苯噻啶在拮抗肌醇磷酸酯1形成方面的活性略低于(2倍)阻断自身受体,而赛庚啶在拮抗两种海马毒蕈碱受体方面的活性相同。