Kavain
Encyclopedia
Kavain is the main kavalactone
found mostly in the root
s of the Kava
plant.
smooth muscle
contraction through interactions with voltage-dependent Na+ and Ca2+ channels. How this effect is mediated and to what extent this mechanism is involved in the anxiolytic
and analgesic
effects of kavalactones on the central nervous system
is unknown. Kavain acting as a serotonin reuptake inhibitor has not been confirmed but monoamine (norepinephrine
) uptake inhibitions and activation of NMDA receptor
s has been noted.
The mechanism behind the psychotropic, sedative
and anxiolytic
actions of kavain and related kavalactones is still debated. Direct binding to the GABAA receptor (benzodiazepine
-receptor) does not occur with kavain enantiomers. Many studies involved kava extracts from different plant parts and are therefore not applicable to kavain itself.
Kavain and analogs without potential hepatotoxic effects remain an interesting target for drug discovery
in the search for novel and less addictive anxiolytics.
Kavalactone
Kavalactones are a class of lactone compounds found in the kava shrub.-Compounds:At least 18 different kavalactones have been identified to date, with methysticin being the first identified.Analogues, such as ethysticin, have also been isolated....
found mostly in the root
Root
In vascular plants, the root is the organ of a plant that typically lies below the surface of the soil. This is not always the case, however, since a root can also be aerial or aerating . Furthermore, a stem normally occurring below ground is not exceptional either...
s of the Kava
Kava
Kava or kava-kava is a crop of the western Pacific....
plant.
Pharmacology
Kavain has anticonvulsive properties, attenuating vascularVascular
Vascular in zoology and medicine means "related to blood vessels", which are part of the circulatory system. An organ or tissue that is vascularized is heavily endowed with blood vessels and thus richly supplied with blood....
smooth muscle
Smooth muscle
Smooth muscle is an involuntary non-striated muscle. It is divided into two sub-groups; the single-unit and multiunit smooth muscle. Within single-unit smooth muscle tissues, the autonomic nervous system innervates a single cell within a sheet or bundle and the action potential is propagated by...
contraction through interactions with voltage-dependent Na+ and Ca2+ channels. How this effect is mediated and to what extent this mechanism is involved in the anxiolytic
Anxiolytic
An anxiolytic is a drug used for the treatment of anxiety, and its related psychological and physical symptoms...
and analgesic
Analgesic
An analgesic is any member of the group of drugs used to relieve pain . The word analgesic derives from Greek an- and algos ....
effects of kavalactones on the central nervous system
Central nervous system
The central nervous system is the part of the nervous system that integrates the information that it receives from, and coordinates the activity of, all parts of the bodies of bilaterian animals—that is, all multicellular animals except sponges and radially symmetric animals such as jellyfish...
is unknown. Kavain acting as a serotonin reuptake inhibitor has not been confirmed but monoamine (norepinephrine
Norepinephrine
Norepinephrine is the US name for noradrenaline , a catecholamine with multiple roles including as a hormone and a neurotransmitter...
) uptake inhibitions and activation of NMDA receptor
NMDA receptor
The NMDA receptor , a glutamate receptor, is the predominant molecular device for controlling synaptic plasticity and memory function....
s has been noted.
The mechanism behind the psychotropic, sedative
Sedative
A sedative or tranquilizer is a substance that induces sedation by reducing irritability or excitement....
and anxiolytic
Anxiolytic
An anxiolytic is a drug used for the treatment of anxiety, and its related psychological and physical symptoms...
actions of kavain and related kavalactones is still debated. Direct binding to the GABAA receptor (benzodiazepine
Benzodiazepine
A benzodiazepine is a psychoactive drug whose core chemical structure is the fusion of a benzene ring and a diazepine ring...
-receptor) does not occur with kavain enantiomers. Many studies involved kava extracts from different plant parts and are therefore not applicable to kavain itself.
Kavain and analogs without potential hepatotoxic effects remain an interesting target for drug discovery
Drug discovery
In the fields of medicine, biotechnology and pharmacology, drug discovery is the process by which drugs are discovered or designed.In the past most drugs have been discovered either by identifying the active ingredient from traditional remedies or by serendipitous discovery...
in the search for novel and less addictive anxiolytics.