ZK-93423
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| 化学式 | C23H22N2O4 |
| 分子量 | 390.44 g·mol−1 |
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ZK-93423は、β-カルボリン系抗不安薬で、アベカルニルと密接に関連がある[1]。非ベンゾジアゼピン系GABAA受容体アゴニストであり、サブタイプ選択性はなく、α1、α2、α3、α5サブユニットを含むGABAA受容体を等しく刺激する[2]。ZK-93423はベンゾジアゼピン系薬物と同等の抗てんかん作用、筋弛緩作用、食欲増進作用を持つ[3][4][5][6]。ZK-93423は、新しい改良されたβ-カルボリン誘導体を開発するためのベースとしても使用されており、GABAA受容体の結合部位のマッピングにも役立っている[7][8][9][10][11][12]。
- ↑ “Synthesis of beta- and gamma-carbolines by the palladium-catalyzed iminoannulation of alkynes”. The Journal of Organic Chemistry 67 (26): 9318–30. (December 2002). doi:10.1021/jo026317u. PMID 12492334.
- ↑ “Discriminative stimulus properties of beta-carbolines characterized as agonists and inverse agonists at central benzodiazepine receptors”. Psychopharmacology 83 (3): 233–9. (1984). doi:10.1007/BF00464787. PMID 6089245.
- ↑ “Evaluation of the muscle relaxant properties of a novel beta-carboline, ZK 93423 in rats and cats”. British Journal of Pharmacology 86 (2): 357–66. (October 1985). doi:10.1111/j.1476-5381.1985.tb08904.x. PMC 1916712. PMID 3931731. https://pmc.ncbi.nlm.nih.gov/articles/PMC1916712/.
- ↑ Cooper SJ (January 1986). “Hyperphagic and anorectic effects of beta-carbolines in a palatable food consumption test: comparisons with triazolam and quazepam”. European Journal of Pharmacology 120 (3): 257–65. doi:10.1016/0014-2999(86)90466-8. PMID 3753939.
- ↑ “Effects of beta-carbolines in animal models of anxiety”. Brain Research Bulletin 19 (3): 293–9. (September 1987). doi:10.1016/0361-9230(87)90097-9. PMID 3315125.
- ↑ “Anticonvulsant efficacy of clonazepam and the beta-carboline ZK 93423 during chronic treatment in amygdala-kindled rats”. European Journal of Pharmacology 143 (3): 403–14. (November 1987). doi:10.1016/0014-2999(87)90464-X. PMID 3691663.
- ↑ “Synthesis of beta-carboline-benzodiazepine hybrid molecules: use of the known structural requirements for benzodiazepine and beta-carboline binding in designing a novel, high-affinity ligand for the benzodiazepine receptor”. Journal of Medicinal Chemistry 30 (7): 1248–54. (July 1987). doi:10.1021/jm00390a023. PMID 3037081.
- ↑ “Structural requirements for agonist actions at the benzodiazepine receptor: studies with analogues of 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester”. Journal of Medicinal Chemistry 33 (3): 1062–9. (March 1990). doi:10.1021/jm00165a028. PMID 1968513.
- ↑ “The agonist pharmacophore of the benzodiazepine receptor. Synthesis of a selective anticonvulsant/anxiolytic”. Journal of Medicinal Chemistry 34 (5): 1754–6. (May 1991). doi:10.1021/jm00109a035. PMID 1674542.
- ↑ “Quantitative structure-activity relationship study of some benzodiazepine-receptor ligands having inverse agonist/antagonist and agonist actions”. Drug Design and Discovery 9 (2): 135–43. (1992). PMID 1338366.
- ↑ “Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) and the full agonist 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (Zk 93423) at wild type and recombinant GABAA receptors”. Journal of Medicinal Chemistry 41 (14): 2537–52. (July 1998). doi:10.1021/jm970460b. PMID 9651158.
- ↑ “Structural features controlling the binding of beta-carbolines to the benzodiazepine receptor”. Acta Crystallographica B 60 (Pt 4): 481–9. (August 2004). doi:10.1107/S0108768104013564. PMID 15258407.
関連項目
| GABAA PAMs |
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| α2δ VDCC Blockers | |||||||||
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| H1 拮抗薬 |
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| CRF1 拮抗薬 | |||||||||
| NK2 拮抗薬 | |||||||||
| MCH1 拮抗薬 | |||||||||
| mGluR2/3 作動薬 | |||||||||
| mGluR5 NAMs | |||||||||
| TSPO 作動薬 | |||||||||
| σ1 作動薬 | |||||||||
| Others | |||||||||
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