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Flavonoid sedatives

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I just found some very recent journal articles about the sedative/GABAergic effects of flavone derivatives...

3-Hydroxy-2'-methoxy-6-methylflavone: a potent anxiolytic with a unique selectivity profile at GABA(A) receptor subtypes.
http://www.ncbi.nlm.nih.gov/pubmed/21924247

2′-Methoxy-6-methylflavone: a novel anxiolytic and sedative with subtype selective activating and modulating actions at GABAA receptors
http://onlinelibrary.wiley.com/doi/10.1111/j.1476-5381.2011.01604.x/abstract

Is this stuff likely to be potent enough to cause a benzo-like 'high' with ataxia, euphoria and amnesia in large doses, or is the potency more like valerian or other herbal remedies?
 
Neurochem Res. 1997 Apr;22(4):419-25.
Overview--flavonoids: a new family of benzodiazepine receptor ligands.
Medina JH, Viola H, Wolfman C, Marder M, Wasowski C, Calvo D, Paladini AC.
Source

Instituto de Biologia Celular y Neurociencias, Facultad de Medicina, UBA, Paraguay, Buenos Aires, Argentina.
Abstract

Benzodiazepines (BDZs) are the most widely prescribed class of psychoactive drugs in current therapeutic use, despite the important unwanted side-effects that they produce such as sedation, myorelaxation, ataxia, amnesia, ethanol and barbiturate potentiation and tolerance. Searching for safer BDZ-receptor (BDZ-R) ligands we have recently demonstrated the existence of a new family of ligands which have a flavonoid structure. First isolated from plants used as tranquilizers in folkloric medicine, some natural flavonoids have shown to possess a selective and relatively mild affinity for BDZ-Rs and a pharmacological profile compatible with a partial agonistic action. In a logical extension of this discovery various synthetic derivatives of those compounds, such as 6,3'-dinitroflavone were found to have a very potent anxiolytic effect not associated with myorelaxant, amnestic or sedative actions. This dinitro compound, in particular, exhibits a high affinity for the BDZ-Rs (Ki = 12-30 nM). Due to their selective pharmacological profile and low intrinsic efficacy at the BDZ-Rs, flavonoid derivatives, such as those described, could represent an improved therapeutic tool in the treatment of anxiety. In addition, several flavone derivatives may provide important leads for the development of potent and selective BDZ-Rs ligands.

PMID:
9130252
Click to expand...

Included in article (quite few publicationson this topic) above but remember reading about Nitro-versions of flavonoids being BZD agonists.
 
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where are those derivatives isolated from ? i cant find any other info than one you provided.
 
tnx for this. i was wondering because i could not recognize those as natural sources :)
 
Flavonoids appear to be active compounds of some sedative and anxiolytic plants.
If you want some examples (you can find many others):
http://www.ncbi.nlm.nih.gov/pubmed/20051259
http://www.ncbi.nlm.nih.gov/pubmed/21788126

As said, they have activities on the GABA system... But, they have activities on the opioid system too:
http://www.ncbi.nlm.nih.gov/pubmed/17685652
Or for Hesperidin:
http://www.ncbi.nlm.nih.gov/pubmed/18048026

I think, we can find very interesting structures for new drugs based on the flavonoids (sleep aids, anxio, pain killer,..). They seem to be quite active, without report of abuse (from the one that could be find through natural sources).
In addition, flavonoids have anti-cancerous and neuro-protectives properties... which is better than a neuro-toxicity :\

One major question is their abilities to go trough the blood-brain-barrier.

I hope it will interest you!
sorry for my poor english
 
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