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Kavalactones and Dihydrokavain Modulate GABAergic Activity in a Rat Gastric-Brainstem Preparation

Kavalactones and Dihydrokavain Modulate GABAergic Activity in a Rat Gastric-Brainstem Preparation

Chun-Su Yuan, Lucy Dey, Anbao Wang, Sangeeta Mehendale, Jing-Tian Xie, Han H Aung, Michael K Ang-Lee

Planta Med. 2002 Dec;68(12):1092-6.

PMID: 12494336

Abstract:

Using an in vitro neonatal rat gastric-brainstem preparation, the activity of majority neurons recorded in the nucleus tractus solitarius (NTS) of the brainstem were significantly inhibited by GABA A receptor agonist, muscimol (30 microM), and this inhibition was reversed by selective GABA A receptor antagonist, bicuculline (10 microM). Application of kavalactones (300 microg/ml) and dihydrokavain (300 microM) into the brainstem compartment of the preparation also significantly reduced the discharge rate of these NTS neurons (39 % and 32 %, respectively, compared to the control level), and this reduction was partially reversed by bicuculline (10 microM). Kavalactones or dihydrokavain induced inhibitory effects were not reduced after co-application of saclofen (10 microM; a selective GABA B receptor antagonist) or naloxone (100 nM; an opioid receptor antagonist). Pretreatment with kavalactones (300 microg/ml) or dihydrokavain (300 microM) significantly decreased the NTS inhibitory effects induced by muscimol (30 microM), approximately from 51 % to 36 %. Our results demonstrated modulation of brainstem GABAergic mechanism by kavalactones and dihydrokavain, and suggested that these compounds may play an important role in regulation of GABAergic neurotransmission.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP587633-B	Dihydrokavain		587-63-3	Price

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