TPA-023 is an anxiolytic drug with a novel chemical structure, which is used in scientific research. It has similar effects to benzodiazepine drugs, but is structurally distinct and so is classed as a nonbenzodiazepine anxiolytic. It is a subtype-selective, mixed agonist-antagonist at GABAA receptors, which acts as a partial agonist at the α2 and α3 subtypes, but as a silent antagonist at α1 and α5 subtypes. It has primarily anxiolytic and anticonvulsant effects in animal tests, but with no sedative effects even at 50× the effective anxiolytic dose.
In human trials on healthy volunteers, TPA-023 was comparable to lorazepam, but had much less side effects on cognition, memory, alertness or coordination. In Phase II trials, the compound was significantly superior to placebo without inducing sedation. The clinical development was halted due to preclinical toxicity (cataract) in long term dosing studies. TPA-023 is well absorbed following oral administration and extensively metabolised by the liver, with a half-life of 6.7 hours. The main enzyme involved in its metabolism is CYP3A4, with some contribution by CYP3A5.
There's war in the heavens
Rebellion on high
the son of the morning
Descends from a black sky
Severed and broken
His wings burned to dust
His coverings of diamonds and gold
In a moment in time dissolve to rust
Thunder and lightning
Shatter the night
The dragon of darkness
Appears cursed by the keeper of the light
The dark is chosen
The scroll has been sealed
Hidden in verses of prophets
His face is revealed
Songs of glory
Shout across the land
I can take you there
Child of mine, take my hand
Down through the ages
The story's been told
The daughter of wisdom
Beguiled by the serpent of old
Born into sin in a valley of thorns
Torn from enchantment and
Tossed into the eye of the storm
Heaven's garden
Made by God for man
This is paradise
Child of mine, take my hand
Glory to glory
Sin after sin
The rider of death
Pushes on to the place where
The battle must begin
Songs of glory
Shout across the land
This is paradise
Won't you take my hand
Heaven's garden
Made by God for man
This is paradise
Child of mine, take my hand
Oh, take my hand