ArticleBritish journal of pharmacology2002
The human 5-HT7 serotonin receptor splice variants: constitutive activity and inverse agonist effects.
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 34 papers.
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Who cites it
34 citing papers in PubMed, 103 citations in OpenAlex.
- Targeting disrupted networks in schizophrenia: Can muscarinic drugs make a fundamental difference?Journal of psychopharmacology (Oxford, England) · 2025Review
- The cell adhesion molecule CD44 acts as a modulator of 5-HT7 receptor functions.Cell communication and signaling : CCS · 2024Article
- Neuroprotective and Neurite Outgrowth Stimulating Effects of New Low-Basicity 5-HTNeurochemical research · 2024Article
- Serotonin Receptors in Myocardial Infarction: Friend or Foe?ACS chemical neuroscience · 2024Review
- β-arrestin biased signaling is not involved in the hypotensive actions of 5-HTPharmacological research · 2024Article
- Investigates the Role of PANoptosis in Idiopathic Pulmonary Fibrosis and Potential Therapeutic Targets.Journal of inflammation research · 2024Article
- Can Serotonin 7 Receptors Be a Treatment Target for Noncentral Diseases?The Eurasian journal of medicine · 2023Article
- 5-HTMicrocirculation (New York, N.Y. : 1994) · 2023Article
- 5-HT7 Receptor Restrains 5-HT-induced 5-HT2A Mediated Contraction in the Isolated Abdominal Vena Cava.Journal of cardiovascular pharmacology · 2021Article
- Effects of Subchronic Administrations of Vortioxetine, Lurasidone, and Escitalopram on Thalamocortical Glutamatergic Transmission Associated with Serotonin 5-HT7 Receptor.International journal of molecular sciences · 2021Article
- International Union of Basic and Clinical Pharmacology. CX. Classification of Receptors for 5-hydroxytryptamine; Pharmacology and Function.Pharmacological reviews · 2021Review
- Ligand-induced activation of ERK1/2 signaling by constitutively active GActa pharmacologica Sinica · 2019Article
- Allosteric Inhibition of Serotonin 5-HTMolecular neurobiology · 2018Article
- Activation of 5-hyrdoxytryptamine 7 receptors within the rat nucleus tractus solitarii modulates synaptic properties.Brain research · 2016Article
- Article
- The atypical antipsychotics clozapine and olanzapine promote down-regulation and display functional selectivity at human 5-HT7 receptors.British journal of pharmacology · 2015Article
- Alternative Splicing of G Protein-Coupled Receptors: Relevance to Pain Management.Mayo Clinic proceedings · 2015Review
- The serotonin 5-HT7 receptors: two decades of research.Experimental brain research · 2013Review
- Effect of methysergide on pudendal inhibition of micturition reflex in cats.Experimental neurology · 2013Article
- Role of the 5-HT7 receptor in the central nervous system: from current status to future perspectives.Molecular neurobiology · 2011Review
Corrections and comments
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Authors and funding
2 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1. Using membranes from stably or transiently transfected HEK293 cells cultured in 5-HT-free medium and expressing the recombinant human 5-HT(7) receptor splice variants (h5-HT(7(a)), h5-HT(7(b)) and h5-HT(7(d))), we compared their abilities to constitutively activate adenylyl cyclase (AC). 2. All h5-HT(7) splice variants elevated basal and forskolin-stimulated AC. The basal AC activity was reduced by the 5-HT(7) antagonist methiothepin and this effect was blocked by mesulergine (neutral 5-HT(7) antagonist) indicating that the inhibitory effect of methiothepin is inverse agonism at the 5-HT(7) receptor. 3. Receptor density correlated poorly with constitutive AC activity in stable clonal cell lines and transiently transfected cells. Mean constitutive AC activity as a percentage of forskolin-stimulated AC was significantly higher for the h5-HT(7(b)) splice variant compared to the h5-HT(7(a)) and h5-HT(7(d)) splice variants but only in stable cell lines. 4. All eight 5-HT antagonists tested inhibited constitutive AC activity of all splice variants in a concentration-dependent manner. No differences in inverse agonist potencies (pIC(50)) were observed between the splice variants. The rank order of potencies was in agreement and highly correlated with antagonist potencies (pK(b)) determined by antagonism of 5-HT-stimulated AC activity (methiothepin >metergoline> mesulergine > or = clozapine > or = spiperone > or = ritanserin > methysergide > ketanserin). 5. The efficacy of inverse agonism was not receptor level dependent and varied for several 5-HT antagonists between membrane preparations of transiently and stably transfected cells. 6. It is concluded that the h5-HT(7) splice variants display similar constitutive activity and inverse agonist properties.
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