Literature DB >> 12138019

GABA(B)-receptor mediation of the inhibitory effect of gamma-hydroxybutyric acid on intestinal motility in mice.

Mauro A M Carai1, Roberta Agabio, Carla Lobina, Roberta Reali, Giovanni Vacca, Giancarlo Colombo, Gian Luigi Gessa.   

Abstract

The effect of acutely administered gamma-hydroxybutyric acid (GHB) and GHB receptor antagonist, NCS-382, on the propulsive activity in the mouse small intestine was assessed by measuring the transit of an orally administered, non absorbable marker. Both GHB (0, 25, 50, 100, 200 and 300 mg/kg; i.p.) and NCS-382 (0, 25, 50 and 75 mg/kg; i.p.) induced a dose-dependent inhibition (up to 50-60%) of the marker transit. Pretreatment with the GABA(B) receptor antagonist, SCH 50911 (100 mg/kg; i.p.), resulted in the blockade of the inhibiting effect of both GHB and NCS-382. These results suggest that the constipating effect of GHB and NCS-382 are secondary to stimulation of the GABA(B) receptor.

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Year:  2002        PMID: 12138019     DOI: 10.1016/s0024-3205(02)01553-9

Source DB:  PubMed          Journal:  Life Sci        ISSN: 0024-3205            Impact factor:   5.037


  5 in total

1.  Toxicologic/transport properties of NCS-382, a γ-hydroxybutyrate (GHB) receptor ligand, in neuronal and epithelial cells: Therapeutic implications for SSADH deficiency, a GABA metabolic disorder.

Authors:  K R Vogel; G R Ainslie; A McConnell; J-B Roullet; K M Gibson
Journal:  Toxicol In Vitro       Date:  2017-10-12       Impact factor: 3.500

2.  Mechanistic toxicokinetic model for gamma-hydroxybutyric acid: inhibition of active renal reabsorption as a potential therapeutic strategy.

Authors:  Melanie A Felmlee; Qi Wang; Dapeng Cui; Samuel A Roiko; Marilyn E Morris
Journal:  AAPS J       Date:  2010-05-12       Impact factor: 4.009

Review 3.  Behavioral analyses of GHB: receptor mechanisms.

Authors:  Lawrence P Carter; Wouter Koek; Charles P France
Journal:  Pharmacol Ther       Date:  2008-10-29       Impact factor: 12.310

4.  Differences in gut microbial composition correlate with regional brain volumes in irritable bowel syndrome.

Authors:  Jennifer S Labus; Emily B Hollister; Jonathan Jacobs; Kyleigh Kirbach; Numan Oezguen; Arpana Gupta; Jonathan Acosta; Ruth Ann Luna; Kjersti Aagaard; James Versalovic; Tor Savidge; Elaine Hsiao; Kirsten Tillisch; Emeran A Mayer
Journal:  Microbiome       Date:  2017-05-01       Impact factor: 14.650

5.  Pharmacokinetics, bioavailability, and bioequivalence of lower-sodium oxybate in healthy participants in two open-label, randomized, crossover studies.

Authors:  Cuiping Chen; Jack Jenkins; Katie Zomorodi; Roman Skowronski
Journal:  Clin Transl Sci       Date:  2021-06-25       Impact factor: 4.689

  5 in total

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