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Analogs of the Musc...
Analogs of the Muscarinic Agent 2'‑Methylspiro(1‑azabicyclo[2.2.2]octane)‑3,4'‑[1,3]dioxolane (AF30) : Synthesis and Pharmacology
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- Nordvall, Gunnar (författare)
- Uppsala universitet,Avdelningen för organisk farmaceutisk kemi
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- Sundquist, Staffan (författare)
- KABI PHARM AB, DEPT RECEPTOR PHARMACOL UROL GYNAECOL, S-11287 STOCKHOLM, SWEDEN
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- Glas, Gunilla (författare)
- KABI PHARM AB, DEPT RECEPTOR PHARMACOL UROL GYNAECOL, S-11287 STOCKHOLM, SWEDEN
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- Gogoll, Adolf (författare)
- Uppsala universitet,Organisk kemi
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- Nilvebrant, Lisbeth (författare)
- KABI PHARM AB, DEPT RECEPTOR PHARMACOL UROL GYNAECOL, S-11287 STOCKHOLM, SWEDEN
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- Hacksell, Uli (författare)
- Uppsala universitet,Avdelningen för organisk farmaceutisk kemi
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(creator_code:org_t)
- 2002-05-01
- 1992
- Engelska.
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Ingår i: Journal of Medicinal Chemistry. - : American Chemical Society (ACS). - 0022-2623 .- 1520-4804. ; 35:9, s. 1541-1550
- Relaterad länk:
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Ämnesord
Stäng
- A number of tetrahydrofuran analogues of 2'-methylspiro[1-azabicyclo[2.2.2]octane-3,4'-[1,3]dioxolane] ( 1) have been prepared with the aim to obtain information about the relative importance of each of the oxygens in 1 for efficacy and for selectivity. In addition, the dimethyl and deamethyl doguea of 1 &re prepared. The new compounds were compared to cis- and trans-1 with regard to their ability to displace (-)-[3H]-3-quinuclidinyl benzilate ((-)-[3H]QNB) from muscarinic receptors in cerebral cortex, heart, parotid gland, and urinary bladder from guinea pigs. Functioinal studies were made on isolated guinea pig bladder and ileum. The new compounds exhibited both lower affmity and efficacy thancis-1.Aconformational studywasperformed,and the effects of steric and electronic factors on the biological activity of the compounds are discussed.
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