Characterization of the 5-HTIB recognition site in rat brain: Binding studies with (−)[125I]Iodocyanopindolol
References (54)
A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding
Anal. Biochem.
(1976)- et al.
The β-adrenergic receptor in human lymphocytes: sub-classification by the use of a new radioligand, (±)-125Iodocyanpindolol
Life Sci.
(1981) [3H]-mesulergine, a selective ligand for serotonin-2 receptors
Life Sci.
(1983)- et al.
A ternary complex model explains the agonist-specific binding properties of the adenylate cyclase-coupled β-adrenergic receptor
J. Biol. Chem.
(1980) - et al.
Biochemical assessment of the central 5-HT agonist activity of RU 24969 (a piperidynylindole)
European J. Pharmacol.
(1980) Mathematical theory of complex ligand-binding system at equilibrium: some methods for parameter fitting
Anal. Biochem.
(1972)- et al.
125I-LSD: a high selectivity ligand for serotonin receptors
European J. Pharmacol.
(1983) - et al.
Molecular pharmacology of 5-HT1 and 5-HT2 recognition sites in rat and pig brain membranes: radioligand binding studies with [3H]5-HT, [3H]8-OH-DPAT, (−)[125I]iodocyanopindolol, [3H]mesulergine and [3H]ketanserin
European J. Pharmacol.
(1985) - et al.
Receptor binding profile of R 41 468, a novel agonist at 5HT2 receptors
Life Sci.
(1981) Stereoselective blockade at [3H]5-HT binding sites and at the 5-HT autoreceptor by propranolol
European J. Pharmacol.
(1984)
8-Hydroxy-2-(di-n-propylamino)-tetralin discriminates subtypes of the 5-HT, recognition site
European J. Pharmacol.
Serotonergic and adrenergic regulation of skeletal muscle metabolism in the rat. II: The use of [125]iodolysergic acid diethylamine and [125I]iodopindolol as probes of sarcolemmal receptor function and specificity
J. Biol. Chem.
Mesulergine, a selective serotonin-2 ligand in the rat cortex, does not label these receptors, in porcine and human cortex: Evidences for species differences on brain serotonin-2 receptors
European J. Pharmacol.
The binding of serotoninergic ligands to the porcine choroid plexus: Characterization of a new type of serotonin recognition site
European J. Pharmacol.
Autoradiographic localisation of 5-HT1 receptors to human and canine basilar arteries
Brain Res.
Serotonin-induced contraction of canine basilar artery: Mediation by 5HT1 receptors
Brain Res.
Binding of 125I-Iodo-hydroxybenzylpindolol to cerebral membranes: association with 5-hydroxytryptamine recognition sites as well as beta-adrenoceptors
Biochem. Pharmacol.
Evidence for 5HT2 receptors mediating contraction in vascular smooth muscle
J. Pharmacol. Exp. Ther.
Visualization of multiple serotonin receptors in the rat brain by autoradiography
Br. J. Pharmacol.
Inhibition of 5-hydroxytryptamine-induced and -amplified human platelet aggregation by ketanserin (R 41-468), a selective 5-HT2-receptor antagonist
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SCTFIT, A computer program for simultaneous analysis of saturation and competition curves
Serotonin recognition sites are labelled in cerebral cortex by the β-adrenoceptor antagonist [125I]hydroxybenzylpindolol
Br. J. Pharmacol.
Identity of inhibitory presynaptic 5-hydroxytryptamine (5-HT) autoreceptors in the rat brain cortex with 5-HT1B binding sites
Naunyn-Schmiedeb. Arch. Pharmakol.
Evidence for common pharmacological properties of [3H]5-hydroxytryptamine binding sites, presynaptic 5-hydroxytryptamine autoreceptors in CNS and inhibitory presynaptic 5-hydroxytryptamine receptors in sympathetic nerves
Naunyn-Schmiedeb. Arch. Pharmakol.
, a new ligand for β-adrenoceptors: Identification and quantitation of subclasses of β-adrenoceptors in guinea pig
Naunyn-Schmiedeb. Arch. Pharmakol.
Identification of 5HT2-receptors on longitudinal muscle of the guinea pig ileum
J. Rec. Res.
2-[125Iodo]LSD, a new ligand for the characterization and localisation of 5-HT2 receptors
Naunyn-Schmiedeb. Arch. Pharmakol.
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2021, Progress in Brain ResearchCitation Excerpt :Using in vivo voltammetry in guinea pig and anesthetized rat, it has been shown that 5-HT1D receptors regulate 5-HT release in the DRN (Davidson and Stamford, 1995; Pineyro and Blier, 1996; Pineyro et al., 1995). In rodents, where brain 5-HT1D as well as 5-HT1B receptors have been detected, superfusion studies performed in midbrain raphe slices indicated that 5-HT1D receptors negatively regulate 5-HT release (Bruinvels et al., 1993; Hoyer et al., 1985; Waeber et al., 1989a, b). This somatodendritic release of 5-HT in rodents, regulated by 5-HT1D receptor, is independent of 5-HT neuronal firing.
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2020, European Journal of PharmacologyClassification and signaling characteristics of 5-HT receptors: toward the concept of 5-HT receptosomes
2020, Handbook of Behavioral NeuroscienceCitation Excerpt :Further studies showed that 5-HT1A receptor stimulation inhibits cAMP production in both hippocampal membranes (De Vivo & Maayani, 1986) and primary neurons (Bockaert, Dumuis, Bouhelal, Sebben, & Cory, 1987; Weiss, Sebben, Kemp, & Bockaert, 1986). In contrast, 5-HT1B receptor corresponded to [3H]-5-HT binding not displaced by spiperone or 8-OH-DPAT and labeled with [125I]-cyanopindolol, a β-adrenergic blocker (Hoyer, Engel, & Kalkman, 1985). We found that this presynaptic receptor is negatively coupled to adenylyl cyclase in substantia nigra (Bouhelal et al., 1988).
Distribution of 5-HT receptors in the central nervous system: an update
2020, Handbook of Behavioral NeuroscienceCitation Excerpt :As stated above, the “history” of the 5-HT1D receptor has been closely related to that of the 5-HT1B receptor. The nomenclature 5-HT1D was first used to denote a receptor present in bovine brain membranes that was labeled with high affinity by [3H]-5-HT in the presence of suitable drugs to block radioligand binding to 5-HT1A and 5-HT2C (at that time called 5-HT1C), and that had a pharmacological profile distinct from 5-HT1A, 5-HT1B, and 5-HT2C receptors (Heuring & Peroutka, 1987); it had been previously reported that the typical rodent 5-HT1B receptor could not be documented in various nonrodent brains, including human brain (Hoyer et al, 1985a, 1986a). A site with these characteristics was also found in other nonrodent species where 5-HT1B was apparently missing and this prompted the idea that rodent 5-HT1B and nonrodent 5-HT1D are in fact species equivalents, but with a different pharmacology (Hoyer & Middlemiss, 1989).
Serotonin receptors nomenclature
2019, The Serotonin System: History, Neuropharmacology, and Pathologyβ<inf>3</inf>-Adrenoceptor agonists for overactive bladder syndrome: Role of translational pharmacology in a repositioning clinical drug development project
2016, Pharmacology and TherapeuticsCitation Excerpt :Standard radioligands for β1- and β2-adrenoceptors such as [3H]-dihydroalprenolol, [3H]-CGP 12,177 or [125I]-iodocyanopindolol have only low affinity for β3-adrenoceptors (Niclauß et al., 2006), implying that the high concentrations required to label β3-adrenoceptors will saturate β1- and β2-adrenoceptors and cause considerable non-specific binding. Moreover, such high concentrations may also bind to non-β-adrenoceptor sites including serotonin receptors (Hoyer et al., 1985a,1985b) and a protein later identified as a member of the TM9SF multi-spanning membrane protein family (Sugasawa et al., 1997, 2001). Finally, low affinity, particularly with [3H]-CGP 12,177 is associated with fast dissociation from the receptor, creating technical challenges in its use.