ArticleBritish journal of pharmacology2010
Functional interactions between 5-HT2A and presynaptic 5-HT1A receptor-based responses in mice genetically deficient in the serotonin 5-HT transporter (SERT).
Article in British journal of pharmacology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
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Who cites it
28 citing papers in PubMed, 50 citations in OpenAlex.
- Role of β-Arrestin2 Signaling in Neuropharmacological Effects of Psychedelic Drugs.ACS chemical neuroscience · 2026Article
- Serotonin Transporter Blockade Reduces the Psychedelic-Like Effects of 4-Methoxy-ACS chemical neuroscience · 2026Article
- Vigilance state dissociation induced by 5-MeO-DMT in mice.Communications biology · 2026Article
- Psilocybin restrains activity-based anorexia in female rats by enhancing cognitive flexibility: contributions from 5-HT1A and 5-HT2A receptor mechanisms.Molecular psychiatry · 2024Article
- Serotonin Transporter (5-Hydroxytryptamine Transporter, SERT, SLC6A4) and Sodium-dependent Reuptake Inhibitors as Modulators of Pain Behaviors and Analgesic Responses.The journal of pain · 2024Review
- Psilocybin for Depression: From Credibility to Feasibility, What's Missing?Pharmaceuticals (Basel, Switzerland) · 2022Article
- Structure-Activity Relationships for Psilocybin, Baeocystin, Aeruginascin, and Related Analogues to Produce Pharmacological Effects in Mice.ACS pharmacology & translational science · 2022Article
- Automated Computer Software Assessment of 5-Hydroxytryptamine 2A Receptor-Mediated Head Twitch Responses from Video Recordings of Mice.ACS pharmacology & translational science · 2022Article
- An ontogenic study of receptor mechanisms by which acute administration of low-doses of methamphetamine suppresses DOI-induced 5-HTBMC neuroscience · 2022Article
- Cardamonin Modulates Neuropathic Pain through the Possible Involvement of Serotonergic 5-HT1A Receptor Pathway in CCI-Induced Neuropathic Pain Mice Model.Molecules (Basel, Switzerland) · 2021Article
- Delayed Antidepressant Efficacy and the Desensitization Hypothesis.ACS chemical neuroscience · 2019Article
- Perturbed Developmental Serotonin Signaling Affects Prefrontal Catecholaminergic Innervation and Cortical Integrity.Molecular neurobiology · 2019Article
- Receptor binding profiles and behavioral pharmacology of ring-substituted N,N-diallyltryptamine analogs.Neuropharmacology · 2018Article
- Evidence for intact 5-HTNeuropharmacology · 2018Article
- Return of the lysergamides. Part IV: Analytical and pharmacological characterization of lysergic acid morpholide (LSM-775).Drug testing and analysis · 2018Article
- Metabotropic GlutamateFrontiers in pharmacology · 2018Article
- Effect of Hallucinogens on Unconditioned Behavior.Current topics in behavioral neurosciences · 2018Review
- Neuronal ablation of p-Akt at Ser473 leads to altered 5-HT1A/2A receptor function.Neurochemistry international · 2014Article
- Serotonin mediation of early memory formation via 5-HT2B receptor-induced glycogenolysis in the day-old chick.Frontiers in pharmacology · 2014Article
- An evaluation of the serotonin system and perseverative, compulsive, stereotypical, and hyperactive behaviors in dopamine transporter (DAT) knockout mice.Psychopharmacology · 2013Article
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Authors and funding
4 authors at 3 institutions in 2 countries.
Funding
Abstract
background and purposeDespite decreased presynaptic 5-HT(1A) and altered 5-HT(2A) receptor function in genetically-deficient serotonin (5-HT) transporter (SERT) mice, the 5-HT(1A) receptor antagonist N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-2-pyridinylcyclohexanecarboxamide maleate salt (WAY 100635) still induced head twitches in these mice, a well-established 5-HT(2A) receptor-mediated response. EXPERIMENTAL APPROACH: Interactions between 5-HT(1A) and 5-HT(2A) receptors were assessed using the head-twitch response following 5-HT(1A) and 5-HT(2A) receptor agonists and antagonists in SERT wild-type (+/+), heterozygous (+/-), and knockout (-/-) mice. The role of brain 5-HT availability in WAY 100635 induced head twitches was also examined. KEY
resultsWAY 100635 induced head twitches in a SERT gene-dose dependent manner, inducing 5-fold more head twitches in SERT -/- versus SERT +/+ mice. In SERT -/- mice, inhibition of 5-HT synthesis with p-chlorophenylalanine (PCPA) markedly depleted tissue 5-HT in all five brain areas examined and abolished WAY 100635 induced head twitches. Further, the selective 5-HT reuptake inhibitor fluvoxamine increased WAY 100635 induced head twitches in SERT +/+ and +/- mice. Head twitches following the 5-HT(2A) receptor agonist (+/-)-2,5-dimethoxy-4-iodophenyl-2-aminopropane (DOI) were robust in SERT +/+ and +/- mice but much reduced in SERT -/- mice. DOI-induced head twitches were decreased by the 5-HT(1A) agonist 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) in SERT +/+ and +/- mice. All drug-induced head twitches were blocked by the 5-HT(2A) receptor antagonist a-Phenyl-1-(2-phenylethyl)-4-piperidinemethanol (MDL 11,939). CONCLUSIONS AND IMPLICATIONS: These data show that indirect activation of 5-HT(2A) receptors via blockade of presynaptic 5-HT(1A) receptors potentiated head-twitch responses, suggesting functional interactions between these receptors, interactions affected by altered 5-HT availability. Our findings strongly support the correlation of WAY 100635 induced head twitches with increased 5-HT availability, induced genetically or pharmacologically.
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