231287-48-2

Upstream product

• 71367-29-8 4-nitro-thiophenol potassium salt 
• 175422-04-5 2,6-dibromo-4-nitropyridine 
• 98027-81-7 2,6-dibromo-4-nitro-pyridine 1-oxide 
• 25373-69-7 2,6-dibromopyridin N-oxide 
• 626-05-1 2,6-Dibromopyridine 

Downstream Products

• 231286-79-6 4-(2-bromo-6-pyrrolidine-1-yl-pyridine-4-sulphonyl)-phenylamine 
• 231286-73-0 4-(2,6-dibromopyridine-4-sulphonyl)-phenylamine 
• 231287-49-3 2,6-dibromo-4-(4-nitrobenzenesulfonyl)-pyridine 

Relevant academic research and scientific papers

Influence of the 5-HT6 receptor on acetylcholine release in the cortex: Pharmacological characterization of 4-(2-bromo-6-pyrrolidin-1-ylpyridine-4-sulfonyl)phenylamine, a potent and selective 5-ht6 receptor antagonist

A small series of aryl pyridyl sulfones has been prepared and investigated for its 5-HT6 receptor binding properties. Thereof, pyrrolidinyl derivative 11 proved to be a very potent (pKi 9) and selective 5-HT6 receptor antagonist. By means of in vivo microdialysis in the frontal cortex and a passive avoidance paradigm, where 11 reversed a scopolamine induced retention deficit, a functional correlation between 5-HT6 receptors and cholinergic neurotransmission could be shown, supporting the therapeutic potential of 5-HT6 receptors in the treatment of cognitive deficits.

BENZOSULFONE DERIVATIVES

The present invention relates to novel compounds of the general formula STR1 wherein R 1 is hydrogen;R. sup.2 is hydrogen, trifluoromethyl or lower alkyl;R 3 is hydrogen or amino; or R 1 and R 2 or R 3 and R 2 taken together are--CH. dbd.CH--CH=CH--;Z is pyrimidin-4-yl, pyridin-4-yl, pyridin-2-yl or phenyl; R 4, R 5 are each independently hydrogen, lower alkyl, trifluoromethyl, halogen, lower alkoxy, nitrilo, amino, lower alkyl-amino, di-lower alkyl-amino, piperazinyl, morpholinyl, pyrrolidinyl, vinyl, C. sub.3-C 6 cycloalkyl, C 3-C 6 cycloalkenyl, t-buthylethinyl, hydroxyalkylethinyl, phenylethinyl, naphthyl, thiophenyl, or phenyl, which may be substituted by halogen, lower alkoxy, lower alkyl, trifluoromethyl or nitro, or a group--NH(CH. sub.2). sub.n NR 6 R 7,--N(CH 3)(CH 2) n NR 6 R. sup.7,--NH(CH 2) n-morpholin-4-yl or--NH(CH 2) n OH; n is 2-4R 6 and R 7 are each independently hydrogen or lower alkyl,and to their pharmaceutically acceptable salts. It has been found that the compounds of formula I possess a selective affinity to 5HT-6 receptors.