Agonist activity of a novel compound, 1-[3-(3,4-methylenedioxyphenoxy)propyl]-4-phenyl piperazine (BP-554), at central 5-HT1A receptors.

@article{Matsuda1989AgonistAO,
  title={Agonist activity of a novel compound, 1-[3-(3,4-methylenedioxyphenoxy)propyl]-4-phenyl piperazine (BP-554), at central 5-HT1A receptors.},
  author={Toshio Matsuda and Yeon Hee Seong and Hiroyuki Aono and Tomoyuki Kanda and Akemichi Baba and K. Saito and Akihiro Tobe and Heitaroh Iwata},
  journal={European journal of pharmacology},
  year={1989},
  volume={170 1-2},
  pages={
          75-82
        }
}
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Interaction of orally administered 5-[3-[((2S)-1,4-benzodioxan-2-ylmethyl)amino]propoxy]-1,3-benzodioxole (MKC-242) with 5-HT1A receptors in rat brain.

Results suggest that orally administered MKC-242 at the low doses that do not show 5-HT1A-receptor-mediated in vivo responses such as the hypothermic effect, adrenocortical effect and the decrease in 5-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) binding passes the blood-brain barrier and subsequently binds to 5- HT1A receptors in rat brain.

Novel benzodioxan derivative, 5-(3-[((2S)-1,4-benzodioxan-2- ylmethyl)amino]propoxy)-1,3-benzodioxole HCl (MKC-242), with a highly potent and selective agonist activity at rat central serotonin1A receptors.

It is suggested that MKC-242 acts as a full and partial agonist at pre- and postsynaptic 5-HT1A receptors, respectively, in the central nervous system.

MKC-242, a novel 5-HT1A receptor agonist, facilitates cortical acetylcholine release by a mechanism different from that of 8-OH-DPAT in awake rats

Antidepressant-like effect by postsynaptic 5-HT1A receptor activation in mice.

p-chlorophenylalanine attenuates the pituitary-adrenocortical response to 5-HT1A receptor agonists in mice.

Postsynaptic 5‐hydroxytryptamine1A receptor activation increases in vivo dopamine release in rat prefrontal cortex

The present results indicate that activation of postsynaptic 5‐HT1A receptors increases dopamine release in a brain region‐specific manner.

Concepts for the design of 5‐HT1A serotonin agonists and antagonists

The accessibility and use of a standard 5‐HT1A agonist radioligand ([3H]8‐hydroxy‐2‐(dipropylaminotetralin) has resulted in the availability of a large amount of binding data on various serotonergic…

Increase of noradrenaline release in the hypothalamus of freely moving rat by postsynaptic 5‐hydroxytryptamine1A receptor activation

The present results suggest that activation of postsynaptic 5‐HT1A receptors increases NA release in the hypothalamus.

Dopamine D2 and serotonin 5-HT1A receptors mediate the actions of aripiprazole in mesocortical and mesoaccumbens transmission

A Brief Summary for 5-HT Receptors

The comprehensive information on 5-HT receptors is summarized in a concise summary with detailed references, which may help the readers for further information excavation.

References

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Central serotonin agonist actions of LY 165163, 1-(m-trifluoromethylphenyl)-4-(p-aminophenylethyl) piperazine, in rats.

Evidence is provided that LY 165163 is a centrally acting serotonin agonist and the increases in hormone concentrations in serum and of dopamine metabolite concentrations in brain were not antagonized by pretreatment with metergoline, a serotonin antagonist.

Biochemical assessment of the central 5-HT agonist activity of RU 24969 (a piperidinyl indole).

Effect of 1-(m-trifluoromethylphenyl)-piperazine on 3H-serotonin binding to membranes from rat brain in vitro and on serotonin turnover in rat brain in vivo.

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

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    The Journal of pharmacology and experimental therapeutics
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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.

The selective labelling of central 5-HT1A receptor binding sites by [3H]5-methoxy-3-(di-n-propylamino)chroman.

Effects of buspirone and its metabolite, 1-(2-pyrimidinyl)piperazine, on brain monoamines and their metabolites in rats.

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  • Biology, Chemistry
    The Journal of pharmacology and experimental therapeutics
  • 1989
Both buspirone and 1- PP increased hypothalamic concentrations of 3-methoxy-4-hydroxyphenylethyleneglycol (MHPG) sulfate, the norepinephrine metabolite, the effect being more pronounced with 1-PP but occurring after doses as low as 0.3 mg/kg s.c. with each compound.

Pharmacology of 5-hydroxytryptamine-1A receptors which inhibit cAMP production in hippocampal and cortical neurons in primary culture.

The results suggest that in mouse embryonic hippocampal neurons, the 5-HT1A receptors, which are negatively coupled to adenylate cyclase, are distinct from the receptor positively coupled to this enzyme, as well as the anxiolytic drugs, ipsapirone and buspirone, which were potent agonists in hippocampusal neurons and competitive antagonists in cortical neurons.

Molecular pharmacology of 5-HT1 and 5-HT2 recognition sites in rat and pig brain membranes: radioligand binding studies with [3H]5-HT, [3H]8-OH-DPAT, (-)[125I]iodocyanopindolol, [3H]mesulergine and [3H]ketanserin.