Detection of a novel serotonin receptor subtype (5-HT1E) in human brain: interaction with a GTP-binding protein.
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Leonhardt S, Herrick-Davis K, Titeler M
Detection of a novel serotonin receptor subtype (5-HT1E) in human brain: interaction with a GTP-binding protein.
J Neurochem. 1989 Aug;53(2):465-71.
- PubMed ID
- 2664084 [ View in PubMed]
- Abstract
[3H]Serotonin (5-hydroxytryptamine, [3H]5-HT) was used as a radioligand probe of brain 5-HT receptors in homogenates of human cortical tissue. Two binding sites were detected in the presence of 1 microM pindolol (to block 5-HT1A and 5-HT1B receptors), and 100 nM mesulergine (to block 5-HT1C and 5-HT2 receptors). One of these sites demonstrated high affinity for 5-carboxyamidotryptamine (5-CT) and ergotamine, consistent with the known pharmacology of the 5-HT1D receptor; the second site demonstrated low affinity for 5-CT and ergotamine. Computer-assisted analyses indicated that both drugs displayed high affinities (Ki values of 1.1 nM and 0.3 nM for 5-CT and ergotamine, respectively) for 55% of the sites and low affinities (Ki values of 910 nM and 155 nM for 5-CT and ergotamine, respectively) for 45% of the sites. To investigate the non-5-HT1D component of the binding, 100 nM 5-CT (to block 5-HT1A, 5-HT1B, and 5-HT1D receptors) was coincubated with [3H]5-HT, membranes, and mesulergine. The remaining [3H]5-HT binding (hereafter referred to as "5-HT1E") displayed high affinity and saturability (KD, 5.3 nM; Bmax, 83 fmol/mg) in human cortical tissue. Competition studies with nonradioactive drugs indicated that, of the drugs tested, 5-CT and ergotamine displayed the highest selectivity for the 5-HT1D site versus the 5-HT1E site.(ABSTRACT TRUNCATED AT 250 WORDS)
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Bopindolol 5-hydroxytryptamine receptor 1B Protein Humans UnknownNot Available Details Pindolol 5-hydroxytryptamine receptor 1B Protein Humans UnknownOther/unknownLigandDetails - Binding Properties
Drug Target Property Measurement pH Temperature (°C) Methysergide 5-hydroxytryptamine receptor 1E Ki (nM) 59 N/A N/A Details