Interaction of arylpiperazines with 5-HT1A, 5-HT1B, 5-HT1C and 5-HT1D receptors: do discriminatory 5-HT1B receptor ligands exist?

@article{Schoeffter2004InteractionOA,
  title={Interaction of arylpiperazines with 5-HT1A, 5-HT1B, 5-HT1C and 5-HT1D receptors: do discriminatory 5-HT1B receptor ligands exist?},
  author={Philippe Schoeffter and Daniel Hoyer},
  journal={Naunyn-Schmiedeberg's Archives of Pharmacology},
  year={2004},
  volume={339},
  pages={675-683}
}
SummaryThe effects of several putative 5-HT1 receptorsubtype selective ligands were investigated in biochemical models for 5-HT1A, 5-HT1B, and 5-HT1D receptors (inhibition of forskolin-stimulated adenylate cyclase activity in calf hippocampus, rat and calf substantia nigra, respectively) and 5-HT1C receptors (stimulation of inositol phosphates production in pig choroid plexus). Following compounds were studied: 5-HT (5-hydroxytryptamine), TFMPP (1-(mtrifluoromethylphenyl)piperazine), mCPP (1-m… Expand
Functional effects of the 5-HT1D receptor antagonist GR 127,935 at human 5-HT1Dα, 5-HT1Dβ, 5-HT1A and opposum 5-HT1B receptors
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Effects of the 5-HT1 receptor agonists DP-5-CT, CGS 12066B, and RU 24969 on plasma adrenaline and glucose levels in the rat
TLDR
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Evidence for a 5-HT1D receptor-mediated hypothermic effect of the alpha 1-adrenoceptor agonist, SDZ NVI-085, in guinea-pigs.
TLDR
SDZ NVI-085-induced hypothermia in guinea-pigs is probably mediated by 5-HT1D receptors. Expand
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TLDR
The5-HT1B selectivity of CP-93,129, and its lack of 5-HT reuptake blocking properties, suggests that the compound compares favourably with other purported 5- HT1B receptor agonists. Expand
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TLDR
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Serotonin 5‐HT1D Receptors
TLDR
5- HT1D receptors are negatively coupled to adenylate cyclase in guinea-pig and calf substantia nigra, and 5-HT1B receptors are positively coupled toAdenylated cyclaseIn rat substantia Nigra, which suggests that the canine basilar artery and saphenous vein, described as models for "5-HT 1-like" receptors, could contain 5- HT 1D receptors. Expand
Trazodone and its active metabolite m-chlorophenylpiperazine as partial agonists at 5-HT1A receptors assessed by [35S]GTPγS binding
TLDR
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. Expand
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References

SHOWING 1-10 OF 69 REFERENCES
5-HT1 and 5-HT2 binding characteristics of some quipazine analogues.
TLDR
The present results suggest that the unsubstituted benzene ring of quipazine, and of its 1-deaza analogue 2-naphthylpiperazine, makes a significant contribution to the binding of these agents to 5- HT2 sites and, more importantly, may account for their 5-HT2 agonist properties. Expand
Relative efficacies of piperazines at the phosphoinositide hydrolysis-linked serotonergic (5-HT-2 and 5-HT-1c) receptors.
TLDR
It is concluded that quipazine and MK-212 are partial agonists at 5-HT-2 receptors in cerebral cortex, whereas 1-NP, TFMPP and MCPP are pure antagonists of the cortical 5- HT-2 receptor. Expand
The 5-hydroxytryptamine 5-HT1D receptor subtype is negatively coupled to adenylate cyclase in calf substantia nigra
TLDR
The results strongly support the contention that 5-HT1D binding sites are negatively coupled to adenylate cyclase in calf substantia nigra. Expand
5-HT-1a and 5-HT-1b selectivity of two phenylpiperazine derivatives: evidence for 5-HT-1b heterogeneity.
The ability of m-trifluoromethylphenylpiperazine (TFMPP) and an N-substituted derivative, LY 165163 (p-NH2-PE-TFMPP), to discriminate 5-HT-1 binding sites labelled by [3H]5-HT is compared in ratExpand
Interactions of isamoltane (CGP 361A), an anxiolytic phenoxypropanolamine derivative, with 5-HT1, receptor subtypes in the rat brain
TLDR
In vivo, isamoltane increased 5-HTP accumulation in rat cortex following central decarboxylase inhibition at doses of 1 and 3 mg/kg i. Expand
Selectivity of serotonergic drugs for multiple brain serotonin receptors. Role of [3H]-4-bromo-2,5-dimethoxyphenylisopropylamine ([3H]DOB), a 5-HT2 agonist radioligand.
The affinities of putative serotonin receptor agonists and antagonists for 5-HT1A, 5-HT1B, 5-HT1C, and 5-HT2 receptors were assayed using radioligand binding assays. The 5-HT1 sites were labeled withExpand
5-HT1B receptors are negatively coupled with adenylate cyclase in rat substantia nigra.
TLDR
The pharmacological profile of the 5- HT receptor mediating the inhibition of adenylate cyclase in substantia nigra indicates that this receptor probably corresponds to 5-HT1B binding sites. Expand
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.
TLDR
The pharmacological profile of 5-HT1A sites in rat and pig cortex appears to be identical; 5- HT1C sites in pig choroid plexus and rat cortex show no differences; it was not possible to label 5-ht1B sites with [125I]CYP in pig brain membranes indicating that like 5,HT2 receptors, 5-TT1 recognition sites show species differences. Expand
5-HT1A-receptors mediate stimulation of adenylate cyclase in rat hippocampus
TLDR
Data support the concept that 5-HT stimulated adenylate cyclase activity in rat hippocampus is mediated by a5-HT1A receptor, as pharmacologically characterised with a series of agonists and antagonists of various structural classes. Expand
Visualization of a novel serotonin recognition site (5-HT1D) in the human brain by autoradiography
TLDR
The localization of a novel serotonin recognition site named 5-HT1D was studied by autoradiography in human postmortem brain material and suggests an involvement of these sites in the mediation of serotoninergic mechanisms in basal ganglia functions and a possible role in brain diseases where these areas are known to be involved. Expand
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