- Synthesis and structure-activity relationship of some 5- [[[(dialkylamino)alkyl]-1-piperidinyl]acetyl]-10,11-dihydro-5H- benzo[b,e][1,4]diazepin-11-ones as M2-selective antimuscarinics
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A series of 5-[[[(dialkylamino)alkyl]-1-piperidinyl]acetyl]-10,11-dihydro- 5H-dibenzo[b,e][1,4]-diazepin-11-ones were prepared as potential M2- selective ligands. The compounds were evaluated for their affinity and selectivity for the muscarinic cholinergic receptor. The best M2-selective antimuscarinic agent studied is 5-[[4-[4-(diethylamino)butyl]-1- piperidinyl]acetyl]-10,11-dihydro-5H-dibenzo[b,e][1,4]diazepin-11-one, which is approximately 10 times more potent at M2 receptors than previously known compounds such as 11-[[4-[4-(diethylamino)butyl]-1-piperidinyl]acetyl]-5,11- dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one (AQ-RA 741).
- Cohen,Baumgold,Jin,De la Cruz,Rzeszotarski,Reba
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p. 162 - 165
(2007/10/02)
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- Synthesis of some quaternary ammonium alkylating agents and their effects on soman-inhibited acetylcholinesterase
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A number of compounds were synthesized and tested for their ability to realkylate the phosphonate anion of 'aged', soman-inhibited acetylcholinesterase. None were found able to do so, but two of the compounds in particular, [2-(4-pyridyl)ethyl]diethylmethylammonium iodide and its 2-isomer, proved able to slow the rate of aging significantly.
- Gray,Platz,Chang,Leverone,Ferrick,Kramer
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p. 111 - 116
(2007/10/02)
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