Dihydrokavain | CAS:587-63-3 | Manufacturer ChemFaces

Dihydrokavain

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Description:

Dihydrokavain may play an important role in regulation of GABAergic neurotransmission, it non-competitively inhibits the specific binding of [3H]-batrachotoxinin-A 20-alpha-benzoate to receptor site 2 of voltage-gated Na+ channels. Dihydrokavain may treat sleep disturbances, as well as stress and anxiety.

Targets:

GABA Receptor | Sodium channel

In vitro:

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

Kavalactones and dihydrokavain modulate GABAergic activity in a rat gastric-brainstem preparation.[Pubmed: 12494336]

METHODS AND RESULTS:
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 %.
CONCLUSIONS:
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.

Dihydrokavain Description

Source:	The roots of Piper methysticum Forst.
Solvent:	Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
Storage:	Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months(2-8C). Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please email to: service@chemfaces.com
After receiving:	The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.

Kinase Assay:

Planta Med. 1998 Jun;64(5):458-9.

Kavain, dihydrokavain, and dihydromethysticin non-competitively inhibit the specific binding of [3H]-batrachotoxinin-A 20-alpha-benzoate to receptor site 2 of voltage-gated Na+ channels.[Pubmed: 9690349]

METHODS AND RESULTS:
The mode of action of the kava pyrones, kavain, Dihydrokavain and dihydromethysticin on the specific binding of [3H]-batrachotoxinin-A 20-alpha-benzoate to epitope 2 of voltage-dependent Na+ channels was investigated by performing saturation experiments in the presence and absence of these kava pyrones. The tested compounds significantly decreased the apparent total number of binding sites (Bmax) for [3H]-batrachotoxinin-A 20-alpha-benzoate (control: 0.5 pmol/mg protein, kava pyrones: 0.2-0.27 pmol/mg protein) with little change in the equilibrium constants (KD) for [3H]-batrachotoxin-A 20-alpha-benzoate (control: 28.2 nM, kava pyrones: 24-31 nM).
CONCLUSIONS:
The results indicate for the kava pyrones a non-competitive inhibition of the specific [3H]-batrachotoxinin-A 20-alpha-benzoate binding to receptor site 2 of voltage-gated Na+ channels.

Product Name	Dihydrokavain
Price:	$288 / 20mg
CAS No.:	587-63-3
Catalog No.:	CFN90536
Molecular Formula:	C₁₄H₁₆O₃
Molecular Weight:	232.27 g/mol
Purity:	>=98%
Type of Compound:	Phenols
Physical Desc.:	Powder
Source:	The roots of Piper methysticum Forst.
Solvent:	Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
Download:	COA MSDS SDF
Similar structural:	Comparison (Web) (SDF)
Guestbook:

Size /Price /Stock	10 mM * 100 uL in DMSO / Inquiry / In-stock 10 mM * 1 mL in DMSO / Inquiry / In-stock
Related Libraries	Inhibitors Compound Library Neuroprotection Compound Library Phenols Compound Library Sodium Channel Inhibitor Library GABA Receptor Inhibitor Library

	1 mg	5 mg	10 mg	20 mg	25 mg
1 mM	4.3053 mL	21.5267 mL	43.0533 mL	86.1067 mL	107.6334 mL
5 mM	0.8611 mL	4.3053 mL	8.6107 mL	17.2213 mL	21.5267 mL
10 mM	0.4305 mL	2.1527 mL	4.3053 mL	8.6107 mL	10.7633 mL
50 mM	0.0861 mL	0.4305 mL	0.8611 mL	1.7221 mL	2.1527 mL
100 mM	0.0431 mL	0.2153 mL	0.4305 mL	0.8611 mL	1.0763 mL

CFN92660	Hispidin	56070-89-4	288.3	C₁₆H₁₆O₅
CFN91561	4-Methyl-6-(3',4'-dihydroxystyryl)-2-pyrone	149947-22-8	260.2	C₁₄H₁₂O₅
CFN90160	Methysticin	20697-20-5	274.27	C₁₅H₁₄O₅
CFN90332	Dihydromethysticin	19902-91-1	276.28	C₁₅H₁₆O₅
CFN97803	Goniothalamin	17303-67-2	200.23	C₁₃H₁₂O₂
CFN92656	Kawain	500-64-1	230.3	C₁₄H₁₄O₃
CFN90149	Desmethoxy yangonin	15345-89-8	228.24	C₁₄H₁₂O₃
CFN92690	p-Hydroxy-5,6-dehydrokawain	39986-86-2	244.2	C₁₄H₁₂O₄
CFN92658	Yangonin	500-62-9	258.3	C₁₅H₁₄O₄
CFN92659	5,6-Dihydroyangonin	3328-60-7	260.3	C₁₅H₁₆O₄