Topic
AR-A000002
About: AR-A000002 is a research topic. Over the lifetime, 11 publications have been published within this topic receiving 266 citations.
Papers
TL;DR: Molecular modeling studies suggest that sarpogrelate is a 5-HT(2A) selective antagonist and is likely to have pharmacological effects beneficial in the treatment of cardiovascular diseases, as well as the signaling linkages of the 5- HT( 2A) receptors and the mode of agonist binding to 5-hydroxytryptamine receptor using data derived from molecular modeling and site-directed mutagenesis.
182 citations
TL;DR: It is concluded that AR-A000002 is a 5-HT1B receptor antagonist that enhances the serotonergic neurotransmission in guinea pig brain and the terminal 5- HT1B autoreceptors are tonically activated under drug-free as well as citalopram conditions.
Abstract: The terminal 5-HT1B autoreceptors have attracted great pharmacological interest since they are potential targets for compounds modifying serotonergic neurotransmission. In the present work the in vivo biochemical properties of AR-A000002 ((R)-N-[5-methyl-8-(4-methylpiperazin-1-yl)-1,2,3,4-tetrahydro-2-naphthyl]-4-morpholinobenzamide), a novel selective 5-HT1B receptor antagonist, are reported.
28 citations
TL;DR: It is concluded that AR-A000002 is a selective high affinity 5HT(1B) receptor ligand that shows partial agonist activity in recombinant systems and behaves as a 5-HT( 1B) receptors antagonist in native tissues.
23 citations
TL;DR: It is concluded that AR-A000002 is a 5-HT1B receptor antagonist, which enhances persistently the serotonergic neurotransmission in guinea pig brain.
Abstract: Rationale
Recently a new 5-hydroxytryptamine1B (5-HT1B)-receptor antagonist, AR-A000002, was described. It was shown that this compound dose dependently increased 5-HT metabolism and release in guinea pig brain following a single injection.
9 citations
TL;DR: The observed effects suggest that this novel and selective high-affinity 5-HT1B/1D receptor antagonist could be used for the treatment of affective disorders.
Abstract: AR-A000002 is a novel and selective high-affinity 5-HT1B/1D receptor antagonist. The compound has been shown to enhance 5-HT turnover in the guinea pig brain in vivo and to increase the extracellular concentration of 5-HT and the metabolite 5-hydroxyindoleacetic acid (5-HIAA) in guinea pig frontal cortex. The observed effects suggest that the compound could be used for the treatment of affective disorders.
The syntheses of labeled AR-A000002 analogues as needed for the further pharmacological evaluation of this selective 5-HT1B/1D antagonist, are described. Copyright © 2004 John Wiley & Sons, Ltd.
6 citations
Related Topics (5)
Performance Metrics
| Year | Papers |
|---|---|
| 2004 | 5 |
| 2003 | 1 |
| 2001 | 5 |