Literature DB >> 2566650

Characterization of [3H]quipazine binding to 5-hydroxytryptamine3 receptors in rat brain membranes.

C M Milburn1, S J Peroutka.   

Abstract

[3H]Quipazine was used to label binding sites in rat brain membranes that display characteristics of a 5-hydroxytryptamine3 (5-HT3) receptor. The radioligand binds with high affinity (KD, 1.2 +/- 0.1 nM) to a saturable population of sites (Bmax, 3.0 +/- 0.4 pmol/g of tissue) that are differentially located in the brain. Specific [3H]quipazine binding is not affected by guanine or adenine nucleotides. ICS 205-930, BRL 43964, Lilly 278584, and zacopride display less than nanomolar affinity for these sites whereas MDL 72222 is approximately one order of magnitude less potent. The pharmacological profile of the binding site is in excellent agreement with that of 5-HT3 receptors characterized in peripheral physiological models. We conclude that [3H]quipazine labels a 5-HT3 receptor in the rat CNS.

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Year:  1989        PMID： 2566650     DOI： 10.1111/j.1471-4159.1989.tb07258.x

Source DB:  PubMed          Journal:  J Neurochem        ISSN： 0022-3042            Impact factor:   5.372


  10 in total

1.  The pharmacological characterization of 5-HT3 receptors in three isolated preparations derived from guinea-pig tissues.

Authors:  A Butler; C J Elswood; J Burridge; S J Ireland; K T Bunce; G J Kilpatrick; M B Tyers
Journal:  Br J Pharmacol       Date:  1990-11       Impact factor: 8.739

2.  5-HT1D receptors inhibit the monosynaptic stretch reflex by modulating C-fiber activity.

Authors:  Ana M Lucas-Osma; Yaqing Li; Katie Murray; Shihao Lin; Sophie Black; Marilee J Stephens; Andrew H Ahn; C J Heckman; Keith K Fenrich; Karim Fouad; David J Bennett
Journal:  J Neurophysiol       Date:  2019-01-09       Impact factor: 2.714

3.  [3H] GR67330, a very high affinity ligand for 5-HT3 receptors.

Authors:  G J Kilpatrick; A Butler; R M Hagan; B J Jones; M B Tyers
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1990-07       Impact factor: 3.000

4.  Molecular size of the 5-HT3 receptor solubilized from NCB 20 cells.

Authors:  R M McKernan; C S Biggs; N Gillard; K Quirk; C I Ragan
Journal:  Biochem J       Date:  1990-08-01       Impact factor: 3.857

5.  Role of serotonin receptors in the effect of sertraline on feeding behaviour.

Authors:  G Grignaschi; R Samanin
Journal:  Psychopharmacology (Berl)       Date:  1993       Impact factor: 4.530

6.  Polysynaptic excitatory postsynaptic potentials that trigger spasms after spinal cord injury in rats are inhibited by 5-HT1B and 5-HT1F receptors.

Authors:  Katherine C Murray; Marilee J Stephens; Michelle Rank; Jessica D'Amico; Monica A Gorassini; David J Bennett
Journal:  J Neurophysiol       Date:  2011-06-08       Impact factor: 2.714

7.  Agonist interactions with 5-HT3 receptor recognition sites in the rat entorhinal cortex labelled by structurally diverse radioligands.

Authors:  J M Barnes; N M Barnes; B Costall; S M Jagger; R J Naylor; D W Robertson; S Y Roe
Journal:  Br J Pharmacol       Date:  1992-02       Impact factor: 8.739

8.  Motoneuron excitability and muscle spasms are regulated by 5-HT2B and 5-HT2C receptor activity.

Authors:  Katherine C Murray; Marilee J Stephens; Edmund W Ballou; Charles J Heckman; David J Bennett
Journal:  J Neurophysiol       Date:  2010-10-27       Impact factor: 2.714

9.  The interaction of RS 25259-197, a potent and selective antagonist, with 5-HT3 receptors, in vitro.

Authors:  E H Wong; R Clark; E Leung; D Loury; D W Bonhaus; L Jakeman; H Parnes; R L Whiting; R M Eglen
Journal:  Br J Pharmacol       Date:  1995-02       Impact factor: 8.739

10.  Characteristics of 5-HT3 binding sites in NG108-15, NCB-20 neuroblastoma cells and rat cerebral cortex using [3H]-quipazine and [3H]-GR65630 binding.

Authors:  N A Sharif; E H Wong; D N Loury; E Stefanich; A D Michel; R M Eglen; R L Whiting
Journal:  Br J Pharmacol       Date:  1991-04       Impact factor: 8.739
  10 in total

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