ArticleBritish journal of pharmacology2000
Characterization of SB-269970-A, a selective 5-HT(7) receptor antagonist.
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 88 papers, 1 of them a synthesis that pooled it.
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Who cites it
88 citing papers in PubMed, 1 synthesis or guideline pooled it, 283 citations in OpenAlex.
- The 5-HT7 receptor system as a treatment target for mood and anxiety disorders: A systematic review.Journal of psychopharmacology (Oxford, England) · 2023Pooled it
- Targeting the 5-HT7 receptor to block influenza virus entry: mechanistic insights and therapeutic potential of SB269970 HCl.Frontiers in microbiology · 2026Article
- Synthesis and evaluation of aporphinoid 5-HTBioorganic & medicinal chemistry letters · 2025Article
- 5-HTCNS neuroscience & therapeutics · 2025Article
- Therapeutic Effects of Pharmacological Modulation of Serotonin Brain System in Human Patients and Animal Models of Fragile X Syndrome.International journal of molecular sciences · 2025Review
- The 5-HT7 receptor contributes to increased hindquarter blood flow caused by skeletal muscle contraction.Journal of cardiovascular pharmacology · 2025Article
- 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
- β-arrestin biased signaling is not involved in the hypotensive actions of 5-HTPharmacological research · 2024Article
- 5-HTMicrocirculation (New York, N.Y. : 1994) · 2023Article
- Therapeutic Potential and Limitation of Serotonin Type 7 Receptor Modulation.International journal of molecular sciences · 2023Review
- 5-HT7 receptors expressed in the mouse parafacial region are not required for respiratory chemosensitivity.The Journal of physiology · 2022Article
- Hyperthermia and Serotonin: The Quest for a "Better Cyproheptadine".International journal of molecular sciences · 2022Review
- Aripiprazole Offsets Mutant ATXN3-Induced Motor Dysfunction by Targeting Dopamine DBiomedicines · 2022Article
- 5-HT Receptors and Temperature Homeostasis.Biomolecules · 2021Review
- Effect of a 5-HT7 Receptor Antagonist on Reversal Learning in the Rat Attentional Set-Shifting Test.ACS chemical neuroscience · 2021Article
- International Union of Basic and Clinical Pharmacology. CX. Classification of Receptors for 5-hydroxytryptamine; Pharmacology and Function.Pharmacological reviews · 2021Review
- 5-HT does not lower blood pressure in the 5-HTPhysiological genomics · 2019Article
- Creation of the 5-hydroxytryptamine receptor 7 knockout rat as a tool for cardiovascular research.Physiological genomics · 2019Article
- The 5-HTPsychopharmacology · 2018Article
28 more citing papers are in PubMed but not listed here.
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14 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The novel 5-HT(7) receptor antagonist, SB-269970-A, potently displaced [(3)H]-5-CT from human 5-HT(7(a)) (pK(i) 8.9+/-0.1) and 5-HT(7) receptors in guinea-pig cortex (pK(i) 8.3+/-0.2). 5-CT stimulated adenylyl cyclase activity in 5-HT(7(a))/HEK293 membranes (pEC(50) 7.5+/-0.1) and SB-269970-A (0.03 - 1 microM) inhibited the 5-CT concentration-response with no significant alteration in the maximal response. The pA(2) (8.5+/-0.2) for SB-269970-A agreed well with the pK(i) determined from [(3)H]-5-CT binding studies. 5-CT-stimulated adenylyl cyclase activity in guinea-pig hippocampal membranes (pEC(50) of 8.4+/-0.2) was inhibited by SB-269970-A (0.3 microM) with a pK(B) (8.3+/-0.1) in good agreement with its antagonist potency at the human cloned 5-HT(7(a)) receptor and its binding affinity at guinea-pig cortical membranes. 5-HT(7) receptor mRNA was highly expressed in human hypothalamus, amygdala, thalamus, hippocampus and testis. SB-269970-A was CNS penetrant (steady-state brain : blood ratio of ca. 0.83 : 1 in rats) but was rapidly cleared from the blood (CLb=ca. 140 ml min(-1) kg(-1)). Following a single dose (3 mg kg(-1)) SB-269970 was detectable in rat brain at 30 (87 nM) and 60 min (58 nM). In guinea-pigs, brain levels averaged 31 and 51 nM respectively at 30 and 60 min after dosing, although the compound was undetectable in one of the three animals tested. 5-CT (0.3 mg kg(-1) i.p.) induced hypothermia in guinea-pigs was blocked by SB-269970-A (ED(50) 2.96 mg kg(-1) i.p.) and the non-selective 5-HT(7) receptor antagonist metergoline (0.3 - 3 mg kg(-1) s.c.), suggesting a role for 5-HT(7) receptor stimulation in 5-CT induced hypothermia in guinea-pigs. SB-269970-A (30 mg kg(-1)) administered at the start of the sleep period, significantly reduced time spent in Paradoxical Sleep (PS) during the first 3 h of EEG recording in conscious rats.
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