Stoll C, Schwarzwälder U, Johann S, Lambrecht G, Hertting G, Feuerstein T J, Jackisch R
Institut für Experimentelle und Klinische Pharmakologie und Toxikologie der Universitaät, Neuropharmakologisches Labor, Hansastrasse 9A, D-79104 Freiburg, Germany.
Neurochem Res. 2003 Apr;28(3-4):413-7. doi: 10.1023/a:1022836315383.
Oxotremorine-induced inhibition of electrically evoked release of 3H-acetylcholine from brain slices preincubated with 3H-choline was used to characterize muscarinic autoreceptors in rabbit hippocampus and caudate nucleus. From the shifts to the right of the concentration-response curves of oxotremorine in the presence of muscarinic receptor antagonists, the following pKB values [95% C.I.] were determined in the hippocampus: tripinamide: 8.7 [8.5, 8.8]; himbacine: 8.4 [8.3, 8.5]; AQ-RA 741: 8.3 [8.2, 8.5]; 4-DAMP: 8.2 [8.0, 8.3]; hexahydrosiladifenidol: 7.4 [7.2, 7.5]; AF-DX 116: 7.3 [7.1, 7.4]; pirenzepine: 6.8 [6.6, 7.0]; and PD102807: 6.3 [6.0, 6.5]. In the caudate nucleus: tripinamide: 9.1 [8.9, 9.2]; 4-DAMP: 8.3 [8.2, 8.5]; himbacine: 8.1 [8.0, 8.2]; AQ-RA 741: 8.1 [8.0, 8.3]; hexahydrosiladifenidol: 7.3 [7.2, 7.4]; AF-DX 116: 7.1 [7.0, 7.2]; pirenzepine: 6.7 [6.6, 6.8]; and PD102807: 6.5 [6.2, 6.8]. These pKB values fit best to literature values for M2 receptors, suggesting that the muscarinic autoreceptor of the rabbit hippocampus and caudate nucleus is the m2 gene product.
用氧化震颤素抑制预先用³H - 胆碱孵育的脑片电诱发的³H - 乙酰胆碱释放，来表征兔海马体和尾状核中的毒蕈碱自身受体。根据在毒蕈碱受体拮抗剂存在下氧化震颤素浓度 - 反应曲线的右移情况，在海马体中确定了以下pKB值[95%置信区间]：曲哌酰胺：8.7 [8.5, 8.8]；樟柳碱：8.4 [8.3, 8.5]；AQ - RA 741：8.3 [8.2, 8.5]；4 - DAMP：8.2 [8.0, 8.3]；六氢硅二苯醚：7.4 [7.2, 7.5]；AF - DX 116：7.3 [7.1, 7.4]；哌仑西平：6.8 [6.6, 7.0]；以及PD102807：6.3 [6.0, 6.5]。在尾状核中：曲哌酰胺：9.1 [8.9, 9.2]；4 - DAMP：8.3 [8.2, 8.5]；樟柳碱：8.1 [8.0, 8.2]；AQ - RA 741：8.1 [8.0, 8.3]；六氢硅二苯醚：7.3 [7.2, 7.4]；AF - DX 116：7.1 [7.0, 7.2]；哌仑西平：6.7 [6.6, 6.8]；以及PD102807：6.5 [6.2, 6.8]。这些pKB值与M2受体的文献值最相符，表明兔海马体和尾状核中的毒蕈碱自身受体是m2基因产物。
