Literature DB >> 11311747

5-HT(6) receptor antagonists: lead optimisation and biological evaluation of N-aryl and N-heteroaryl 4-amino-benzene sulfonamides.

M Bös1, A J Sleight, T Godel, J R Martin, C Riemer, H Stadler.   

Abstract

RO-04-6790 (6a) has been identified in a random screen for 5-HT(6) receptor antagonists. In a medicinal chemistry optimisation program a series of analogs comprising N-heteroaryl- and N-arylbenzenesulfonamides have been synthesised and investigated for their binding affinity. Compounds with a logD profile indicative of brain penetration have been subjected to in vivo testing for reversal of a scopolamine-induced retention deficit in a passive avoidance paradigm.

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Year:  2001        PMID: 11311747     DOI: 10.1016/s0223-5234(00)01209-5

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  6 in total

Review 1.  Alzheimer's disease and age-related memory decline (preclinical).

Authors:  Alvin V Terry; Patrick M Callahan; Brandon Hall; Scott J Webster
Journal:  Pharmacol Biochem Behav       Date:  2011-02-24       Impact factor: 3.533

2.  Salicylic acid, an ambimobile molecule exhibiting a high ability to accumulate in the phloem.

Authors:  Françoise Rocher; Jean-François Chollet; Cyril Jousse; Jean-Louis Bonnemain
Journal:  Plant Physiol       Date:  2006-06-15       Impact factor: 8.340

3.  Efficacy of selective 5-HT6 receptor ligands determined by monitoring 5-HT6 receptor-mediated cAMP signaling pathways.

Authors:  Gonzalo Romero; Elisabeth Sánchez; Marta Pujol; Pilar Pérez; Xavier Codony; Jörg Holenz; Helmut Buschmann; Petrus J Pauwels
Journal:  Br J Pharmacol       Date:  2006-07-24       Impact factor: 8.739

4.  Reversal of a cholinergic-induced deficit in a rodent model of recognition memory by the selective 5-HT6 receptor antagonist, Ro 04-6790.

Authors:  Marie L Woolley; Charles A Marsden; Andrew J Sleight; Kevin C F Fone
Journal:  Psychopharmacology (Berl)       Date:  2003-09-10       Impact factor: 4.530

5.  Impact of regional 5-HT depletion on the cognitive enhancing effects of a typical 5-ht(6) receptor antagonist, Ro 04-6790, in the Novel Object Discrimination task.

Authors:  M V King; C H Spicer; A J Sleight; C A Marsden; K C F Fone
Journal:  Psychopharmacology (Berl)       Date:  2008-10-07       Impact factor: 4.530

6.  5-HT(6) receptor agonists and antagonists enhance learning and memory in a conditioned emotion response paradigm by modulation of cholinergic and glutamatergic mechanisms.

Authors:  S Woods; N N Clarke; R Layfield; K C F Fone
Journal:  Br J Pharmacol       Date:  2012-09       Impact factor: 8.739

  6 in total

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