The brain serotonin (5-hydroxytryptamine; 5-HT) system is a powerful modulator of emotional processes and a target of medications used in the treatment of psychiatric disorders. To evaluate the contribution of serotonin 5-HT1A receptors to the regulation of these processes, we have used gene-targeting technology to generate 5-HT1A receptor-mutant mice. These animals lack functional 5-HT1A recep...

Single treatment with the serotonin (5-hydroxytryptamine) 5-HT1A receptor agonists 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) and alnespirone (S-20499) reduces the extracellular 5-HT concentration (5-HText) in the rat midbrain and forebrain. Given the therapeutic potential of selective 5-HT1A agonists in the treatment of affective disorders, we have examined the changes in 5-HT1A recept...

A series of 15 new 2-H- and 2-substituted 5-[omega-[4-(2-methoxyphenyl)-piperazinyl]-alkyl]-1,2,3,4-tetrahydro-gamma-carboline derivatives were prepared, and their affinity for 5-HT1A and 5-HT2A serotonin receptors was determined. Most of those hybrid compounds were found to bind with high affinity to 5-HT1A sites (Ki < 50 nM; 2d, 3a, 3b, 3d, 3e, 4b, 4d, 4e) and moreover two of them (4d, 4e) we...

The human 5-hydroxytryptamine 5-HT1A receptor gene was transfected into Chinese hamster ovary cells. A series of recombinant monoclonal cell lines expressing the receptor were isolated and the properties of one cell line that expressed receptors at a high level (2.8 pmol/mg) were studied in detail. In ligand binding assays with the selective 5-HT1A receptor agonist 2-(NN-di[3H]propylamino)-8-hy...

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PURPOSE To assess the neuroprotective effects of flibanserin (formerly BIMT-17), a dual 5-HT1A agonist and 5-HT2A antagonist, in a light-induced retinopathy model. METHODS Albino BALB/c mice were injected intraperitoneally with either vehicle or increasing doses of flibanserin ranging from 0.75 to 15 mg/kg flibanserin. To assess 5-HT1A-mediated effects, BALB/c mice were injected with 10 mg/kg...

Arif Siddiqui, Saeeda Shaharyar Department of Biological and Biomedical Sciences, The Aga Khan University, Karachi. Pakistan Background: The present study was designed to inves tigate the role of the 5-HT7 receptors in lordosis and release of LH and compare the lordotic responses with 5-HT1A agent. Methods: Ovariectomised but oestradiol benzoate (OB) (10 ug) for 48 h plus by progesterone (0.5 m...

Neuronal nitric oxide synthase (nNOS) plays a role in synaptic potentiation and kindling process.The relationship between nNOS and 5-HT1A receptors also nearly has been specified. In this research,we investigate the role of nNOS on the anticonvulsant effect of 5-HT1A receptors. 24 male (280 &plusmn; 30 g) were randomly assigned to four groups (vehicle,NI,Way 100635 and NI + Way100635) (n = 6). ...