Analysis of tandospirone (SM-3997) interactions with neurotransmitter receptor binding sites

  title={Analysis of tandospirone (SM-3997) interactions with neurotransmitter receptor binding sites},
  author={Anne Hamik and Donna Oksenberg and Christine T. Fischette and Stephen J. Peroutka},
  journal={Biological Psychiatry},

In vivo drug action of tandospirone at 5-HT1A receptor examined using positron emission tomography and neuroendocrine response

Despite the significant effect on growth hormone and body temperature, a clinical dose of tandospirone had a negligible effect on [11C]WAY 100635 binding, which indicates that the agonist produces a pharmacological effect without measurable occupancy, and a new index other than occupancy will be required for the in vivo evaluation of agonists.

Tandospirone suppresses impulsive action by possible blockade of the 5-HT1A receptor.

Tandospirone could be a therapeutic candidate for impulsivity-related disorders and may be due to the antagonistic action of the 5-HT1A receptor.

Trazodone and its active metabolite m-chlorophenylpiperazine as partial agonists at 5-HT1A receptors assessed by [35S]GTPγS binding

The agonist properties of trazodone and its active metabolite, m-chlorophenylpiperazine (m-CPP), at 5-HT1A receptors are elucidated by means of the guanosine-5′-O-(3-[ 35S]thio)-triphosphate ([35S]GTPγS) binding assay.

The activity of the serotonergic 5-HT1A receptor is modulated by voltage and sodium levels

Tandospirone activates neuroendocrine and ERK (MAP kinase) signaling pathways specifically through 5-HT1A receptor mechanisms in vivo

The results are the first evidence that systemic 5-HT1A receptor agonist administration produces a rapid increase in p-ERK levels in vivo, providing further insight into the signaling mechanisms of the 5- HT1A receptors.



Interaction of SM-3997 with serotonin receptors in rat brain.

Results suggest that the action of SM-3997 may be mediated via central 5-HT1A receptors but not the BZ-GABA receptor complex.

Identification of presynaptic serotonin autoreceptors using a new ligand: 3H-PAT

3H-PAT seems to be a useful ligand for studying the biochemical and pharmacological characteristics of presynaptic autoreceptors in selected regions of rat brain.

Characterization of the 5-hydroxytryptamine1a receptor-mediated inhibition of forskolin-stimulated adenylate cyclase activity in guinea pig and rat hippocampal membranes.

  • M. De VivoS. Maayani
  • Biology, Chemistry
    The Journal of pharmacology and experimental therapeutics
  • 1986
The concentration-response data show that the inhibition of forskolin-stimulated adenylate cyclase activity in guinea pig and rat hippocampal membranes is mediated by a receptor with the characteristics of the 5-HT1A binding site, and it is proposed that this response is suitable for measuring activities and affinities of drugs acting at 5- HT1A receptors.

Pharmacological properties of SM-3997: a new anxioselective anxiolytic candidate.

The results show that SM-3997 is a new anxioselective anxiolytic agent which is weaker than buspirone in the dopaminergic neuron system.

Selective antagonists of benzodiazepines

The main properties of a representative of this novel class of specific benzodiazepine antagonists are described, whose unique pharmacological activity is to prevent or abolish in a highly selective manner at the receptor level all the characteristic centrally mediated effects of active Benzodiazepines.

Buspirone analogues. 2. Structure-activity relationships of aromatic imide derivatives.

Several analogues of the novel anxiolytic buspirone were synthesized and evaluated in vivo for tranquilizing activity and their ability to reverse neuroleptic-induced catalepsy and general structure-activity relationships highlight compounds 17, 21, and 32 as having anticonflict activity.