Rostom, Sherif A. F. and Farghaly, Ahmed M. and Soliman, Farid S. G. and El-Semary, Mona M. and Elz, Sigurd and Lehmann, Jochen (2001) Synthesis and 5-HT2A antagonist activity of derivatives of the novel heterocycles indolo[3,2-d]pyrrolo[3,2-g]azecine and benzo[d]pyrrolo[3,2-g]azecine compared to the benz[d]indolo[2,3-g]azecine derivative LE 300. ARCHIV DER PHARMAZIE, 334 (7). pp. 241-247. ISSN 0365-6233
Full text not available from this repository. (Request a copy)Abstract
An indolo[3,2-d]pyrrolo[3,2-g]azecine and a benzo[d]pyrrolo[3,2-glazecine analogue of the potent dopamine receptor antagonist LE 300 {7-methyl-6,7,8,9,14,15-hexahydro-5H-benz[d]indolo[2,3-g]azecine) have been prepared in mufti-step reactions via C-N bond cleavage of corresponding quaternary N-methylquinolizinium iodides. LE 300, the target compounds and two precursor quinolizines have been tested in vitro for antagonist activity at 5-HT2A receptors (rat tail artery) and Hl receptors {guinea-pig ileum), respectively. LE 300 and compound 19 {3,6-dimethyl-4,5,6,7,8,13-hexahydro-3H-benzo[d]pyrrolo[3,2-glazecine) competitively inhibited S-HT-induced contractions with similar nanomolar potency (pA(2) = 8.32 and 8.01, respectively) but were less active than the reference antagonist ketanserin (pA(2) = 9.55). Compound 19 displayed moderate H-1-antihistaminic activity in the guinea-pig ileum assay (pA(2) = 7.37).
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | RECEPTOR-BINDING; SEROTONIN; PHARMACOLOGY; INDOLES; LIGAND; azecines; serotonin; histamine antagonists; 5-HT2A-receptor antagonists; LE 300 |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry I (Prof. Elz) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 21 Dec 2021 08:11 |
| Last Modified: | 21 Dec 2021 08:11 |
| URI: | https://pred.uni-regensburg.de/id/eprint/41270 |
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