ArticleBritish journal of pharmacology2000
[(3)H]-SB-269970--A selective antagonist radioligand for 5-HT(7) receptors.
Article in British journal of pharmacology, 2000. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 71 citations in OpenAlex.
- Identification and Pharmacological Characterization of Two Serotonin Type 7 Receptor Isoforms fromInternational journal of molecular sciences · 2022Article
- Mitochondrial Membranes of Human SH-SY5Y Neuroblastoma Cells Express Serotonin 5-HTInternational journal of molecular sciences · 2020Article
- An inactive receptor-G protein complex maintains the dynamic range of agonist-induced signaling.Proceedings of the National Academy of Sciences of the United States of America · 2020Article
- Article
- Allosteric Inhibition of Serotonin 5-HTMolecular neurobiology · 2018Article
- 5-HT3 Receptors: A Potential Therapeutic Target for Epilepsy.Current neuropharmacology · 2018Review
- Activation of 5-hyrdoxytryptamine 7 receptors within the rat nucleus tractus solitarii modulates synaptic properties.Brain research · 2016Article
- The arylpiperazine derivatives N-(4-cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide and N-benzyl-4-(2-diphenyl)-1-piperazinehexanamide exert a long-lasting inhibition of human serotonin 5-HT7 receptor binding and cAMP signaling.Pharmacology research & perspectives · 2013Article
- The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptors.British journal of pharmacology · 2013Article
- The antinociceptive effect of milnacipran in the monosodium iodoacetate model of osteoarthritis pain and its relation to changes in descending inhibition.The Journal of pharmacology and experimental therapeutics · 2013Article
- Alternative approaches to modeling hereditary dystonias.Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics · 2012Review
- Risperidone-induced inactivation and clozapine-induced reactivation of rat cortical astrocyte 5-hydroxytryptamine₇ receptors: evidence for in situ G protein-coupled receptor homodimer protomer cross-talk.Molecular pharmacology · 2011Article
- Acute Ca(2+)-dependent desensitization of 5-HT(1A) receptors is mediated by activation of protein kinase A (PKA) in rat serotonergic neurons.Neuroscience · 2010Article
- The 5-HT(7) receptor as a mediator and modulator of antidepressant-like behavior.Behavioural brain research · 2010Article
- Brown adipose tissue sympathetic nerve activity is potentiated by activation of 5-hydroxytryptamine (5-HT)1A/5-HT7 receptors in the rat spinal cord.Neuropharmacology · 2008Article
- A 5-HT7 heteroreceptor-mediated inhibition of [3H]serotonin release in raphe nuclei slices of the rat: evidence for a serotonergic-glutamatergic interaction.Neurochemical research · 2004Article
- Autoradiographic distribution of 5-HT7 receptors in the human brain using [3H]mesulergine: comparison to other mammalian species.British journal of pharmacology · 2004Article
- SB-656104-A, a novel selective 5-HT7 receptor antagonist, modulates REM sleep in rats.British journal of pharmacology · 2003Article
- Pharmacological characterization of the 5-HT receptors mediating contraction and relaxation of canine isolated proximal stomach smooth muscle.British journal of pharmacology · 2002Article
- SB-258741: a 5-HT7 receptor antagonist of potential clinical interest.CNS drug reviews · 2002Review
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Authors and funding
9 authors at 2 institutions in 2 countries.
Funding
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Abstract
Binding of the 5-HT(7) receptor antagonist radioligand [(3)H]-SB-269970 to human 5-HT(7(a)) receptors expressed in HEK293 cell membranes (h5-HT(7(a))/293) and to guinea-pig cerebral cortex membranes, was characterized and compared with [(3)H]-5-CT binding. [(3)H]-SB-269970 (1 nM) showed full association with h5-HT(7(a))/293 membranes after 40 min. Specific binding at equilibrium represented >90% of total binding and was fully reversible by methiothepin (10 microM), full dissociation occurring by 100 min. The association (k(+1)) and dissociation (k(-1)) rate constants were 0.05 nM(-1)min(-1) and 0.05 min(-1) respectively, giving a K(D) (k(-1)/k(+1)) of 1.0 nM. [(3)H]-SB-269970 bound saturably and apparently monophasically to both h5-HT(7(a))/293 and guinea-pig cortex membranes, with K(D) values of 1.25+/-0.05 and 1.7+/-0.3 nM respectively. The B(max) for [(3)H]-SB-269970 to both h5-HT(7(a))/293 and guinea-pig cortex membranes (5780+/-380 and 125+/-8.2 fmoles mg protein(-1) respectively) was similar to that for [(3)H]-5-CT (6190+/-940 and 143+/-19 fmoles mg protein(-1) respectively). These data suggest that, in each tissue, both radioligands labelled the same population of receptors, which appear to be present in an agonist high affinity state. The profile of compound inhibition of [(3)H]-SB-269970 binding to h5-HT(7(a))/293 and guineapig cortex membranes correlated well (corr. coeff. 0.98) with those for [(3)H]-5-CT binding and were consistent with the profiles reported previously for the human 5-HT(7(a)) and guinea-pig cortex 5-HT(7) receptors using [(3)H]-5-CT. Hill slopes for inhibition of [(3)H]-SB-269970 and [(3)H]-5-CT binding were close to 1, consistent with binding to a single receptor population in both tissues. [(3)H]-SB-269970 represents the first selective 5-HT(7) antagonist radioligand, which should aid further characterization of 5-HT(7) receptors in recombinant and native tissues and help establish their role in brain function.
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