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Literature DB >> 12646038

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.

Claus Riemer¹, Edilio Borroni, Bernard Levet-Trafit, James R Martin, Sonia Poli, Richard H P Porter, Michael Bös.

Abstract

A small series of aryl pyridyl sulfones has been prepared and investigated for its 5-HT(6) receptor binding properties. Thereof, pyrrolidinyl derivative 11 proved to be a very potent (pK(i) 9) and selective 5-HT(6) 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-HT(6) receptors and cholinergic neurotransmission could be shown, supporting the therapeutic potential of 5-HT(6) receptors in the treatment of cognitive deficits.

Entities: Chemical Disease

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Year: 2003 PMID： 12646038 DOI： 10.1021/jm021085c

Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446

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Cited

30 in total

1. Distribution of serotonin receptor of type 6 (5-HT₆) in human brain post-mortem. A pharmacology, autoradiography and immunohistochemistry study.

Authors: Donatella Marazziti; Stefano Baroni; Andrea Pirone; Gino Giannaccini; Laura Betti; Lara Schmid; Elena Vatteroni; Lionella Palego; Franco Borsini; Fabio Bordi; Ilaria Piano; Claudia Gargini; Maura Castagna; Mario Catena-Dell'osso; Antonio Lucacchini
Journal: Neurochem Res Date: 2012-01-26 Impact factor: 3.996

Review 2. Spontaneous object recognition and its relevance to schizophrenia: a review of findings from pharmacological, genetic, lesion and developmental rodent models.

Authors: L Lyon; L M Saksida; T J Bussey
Journal: Psychopharmacology (Berl) Date: 2011-11-10 Impact factor: 4.530

3. Co-administration of 5-HT6 receptor antagonists with clozapine, risperidone, and a 5-HT2A receptor antagonist: effects on prepulse inhibition in rats.

Authors: Katarzyna Fijał; Piotr Popik; Agnieszka Nikiforuk
Journal: Psychopharmacology (Berl) Date: 2013-08-18 Impact factor: 4.530

Review 4. 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

5. Central nervous system effects of the interaction between risperidone (single dose) and the 5-HT6 antagonist SB742457 (repeated doses) in healthy men.

Authors: Marieke Liem-Moolenaar; Mandana Rad; Stefano Zamuner; Adam F Cohen; Francesca Lemme; Kari L Franson; Joop M A van Gerven; Emilio Merlo Pich
Journal: Br J Clin Pharmacol Date: 2011-06 Impact factor: 4.335

6. 5-HT6 receptor blockade differentially affects scopolamine-induced deficits of working memory, recognition memory and aversive learning in mice.

Authors: Virginie Da Silva Costa-Aze; Anne Quiedeville; Michel Boulouard; François Dauphin
Journal: Psychopharmacology (Berl) Date: 2012-02-25 Impact factor: 4.530

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.

1. Distribution of serotonin receptor of type 6 (5-HT₆) in human brain post-mortem. A pharmacology, autoradiography and immunohistochemistry study.

Review 2. Spontaneous object recognition and its relevance to schizophrenia: a review of findings from pharmacological, genetic, lesion and developmental rodent models.

3. Co-administration of 5-HT6 receptor antagonists with clozapine, risperidone, and a 5-HT2A receptor antagonist: effects on prepulse inhibition in rats.

Review 4. Alzheimer's disease and age-related memory decline (preclinical).

5. Central nervous system effects of the interaction between risperidone (single dose) and the 5-HT6 antagonist SB742457 (repeated doses) in healthy men.

6. 5-HT6 receptor blockade differentially affects scopolamine-induced deficits of working memory, recognition memory and aversive learning in mice.

7. The effects of PRX-07034, a novel 5-HT6 antagonist, on cognitive flexibility and working memory in rats.

8. Dorsomedial prefrontal cortex 5-HT6 receptors regulate anxiety-like behavior.

9. Antidepressant and anxiolytic effects of selective 5-HT6 receptor agonists in rats.

10. Effects of 5-HT6 receptor antagonism and cholinesterase inhibition in models of cognitive impairment in the rat.