ArticleBritish journal of pharmacology2002
Differential coupling of 5-HT(1) receptors to G proteins of the G(i) family.
Article in British journal of pharmacology, 2002. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed, 57 citations in OpenAlex.
- Bilobalide increases SKBMC complementary medicine and therapies · 2026Article
- Potential Roles of G Protein-Coupled Receptor 30 (GPR30) in Migraine Pathophysiology.Journal of pain research · 2026Review
- Angiotensin II and EDH Pathways Underlie the Vascular Sympatho-Modulation by 5-HT in Female Rats.International journal of molecular sciences · 2025Article
- Structural determinants of G protein subtype selectivity at the serotonin receptor 5-HT1A.Science advances · 2025Article
- Development of 2-Aminotetralin-Type Serotonin 5-HTACS chemical neuroscience · 2024Article
- Captive ERVWE1 triggers impairment of 5-HT neuronal plasticity in the first-episode schizophrenia by post-transcriptional activation of HTR1B in ALKBH5-m6A dependent epigenetic mechanisms.Cell & bioscience · 2023Article
- 5-HTiScience · 2023Article
- Exploring the Role of Serotonin as an Immune Modulatory Component in Cardiovascular Diseases.International journal of molecular sciences · 2023Review
- The selective 5-HTPsychopharmacology · 2021Article
- Inflammation induces developmentally regulated sumatriptan inhibition of spinal synaptic transmission.British journal of pharmacology · 2020Article
- S-nitrosoglutathione inhibits cerebrovascular angiotensin II-dependent and -independent ATBritish journal of pharmacology · 2019Article
- Article
- 5-HT3 Receptors: A Potential Therapeutic Target for Epilepsy.Current neuropharmacology · 2018Review
- Structure and function of serotonin G protein-coupled receptors.Pharmacology & therapeutics · 2015Review
- 5-Hydroxytryptamine1A receptor-activation hyperpolarizes pyramidal cells and suppresses hippocampal gamma oscillations via Kir3 channel activation.The Journal of physiology · 2014Article
- Bi-allelic and tri-allelic 5-HTTLPR polymorphisms and triptan non-response in cluster headache.The journal of headache and pain · 2014Article
- How much do we know about the coupling of G-proteins to serotonin receptors?Molecular brain · 2014Review
- Serotonin 1A receptor agonist increases species- and region-selective adult CNS proliferation, but not through CNTF.Neuropharmacology · 2012Article
- Serotonin and CGRP in migraine.Annals of neurosciences · 2012Review
- Regulation of dorsal raphe nucleus function by serotonin autoreceptors: a behavioral perspective.Journal of chemical neuroanatomy · 2011Review
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
1: Since all 5-HT(1) receptors couple to G(i)-type G proteins and inhibit adenylyl cyclase, the functional significance of five distinct subtypes of 5-HT(1) receptors has been unclear. 2: In previous studies we have used transfected cells to demonstrate that 5-HT(1B) receptors can couple more efficiently than 5-HT(1A) receptors to activation of extracellular signal-regulated kinase (ERK) and to inhibition of adenylyl cyclase. These findings suggested the possibility that individual 5-HT(1) receptors differentially couple to isoforms of G(ialpha). 3: In the present study we utilized a model system in which pertussis toxin resistant forms of human G(ialpha1), G(ialpha2), and G(ialpha3) were used to directly compare the coupling of human 5-HT(1A), 5-HT(1B), and 5-HT(1D) receptors to each G(ialpha) in transfected human HeLa cells. 4: 5-HT(1A) receptors displayed a preference for G(ialpha1) and G(ialpha2), relative to G(ialpha3). Pertussis toxin resistant forms of G(ialpha1), G(ialpha2), and G(ialpha3) rescued 73%, 76%, and 44%, respectively, of the ERK activation stimulated by 5-HT in the absence of pertussis toxin. 5: In contrast, pertussis toxin resistant forms of G(ialpha1), G(ialpha2), and G(ialpha3) rescued 32%, 118%, and 35% of 5-HT(1B) receptor-stimulated activity, respectively, indicating that 5-HT(1B) receptors coupled primarily through G(ialpha2). A similar preference for G(ialpha2) was found in studies of the 5-HT(1D) receptor, where toxin resistant G(ialpha1), G(ialpha2), and G(ialpha3) rescued 30%, 70%, and 40% of activity, respectively. 6: In conclusion, the observed differential coupling of 5-HT(1) receptors to isoforms of G(ialpha), provides additional evidence for our previous findings that the subtypes of 5-HT(1) receptors exhibit similar, but distinct, functions.
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