Eptapirone

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Eptapirone
File:Eptapirone.png
Systematic (IUPAC) name
4-methyl-2-[4-(4-pyrimidin-2-ylpiperazin-1-yl)butyl]-1,2,4-triazine-3,5-dione
Clinical data
Routes of
administration		 Oral
Legal status
Legal status
  • Uncontrolled
Pharmacokinetic data
Biological half-life ~2 hours
Identifiers
CAS Number 179756-85-5
ATC code none
PubChem CID 208928
ChemSpider 181024
Chemical data
Formula C16H23N7O2
Molar mass 345.40 g/mol[[Script error: No such module "String".]]
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Eptapirone (F-11,440) is a very potent and highly selective 5-HT1A receptor full agonist of the azapirone class.[1][2] Its affinity for the 5-HT1A receptor is 4.8 nM (Ki) or 8.33 (pKi), and its intrinsic activity is 100% or equal to that of serotonin.[1]

Eptapirone and its relatives such as F-13,640 and F-15,599 were developed under the notion that high receptor-activating efficacy is required for the maximal therapeutic benefits of 5-HT1A receptor agonists to be realized, underlying the poor clinical effectiveness of currently marketed agents like buspirone and tandospirone which act as mere weak-moderate partial agonists.[1][3][2][4]

Rodent studies

In the forced swim test, eptapirone suppresses immobility more robustly than buspirone, ipsapirone, flesinoxan, paroxetine, and imipramine, indicating that it possesses powerful antidepressant effects which may be superior to those of currently available pharmaceuticals.[1] In this test, unlike the other agents screened, buspirone actually increases immobility time with a single administration, while repeated administration decreases it, likely as a result of buspirone's very poor intrinsic activity (~30%) in activating the 5-HT1A receptor.[1]

While high dose paroxetine is able to rival the reduction in immobility induced by eptapirone, it is only able to do so after repeated administration (in contrast to eptapirone which requires only a single dose), suggesting that eptapirone has a more rapid onset of action than other antidepressants as well.[1] Imipramine was unable to match eptapirone or high dose paroxetine's efficacy as greater doses were fatal.[1]

In the conflict procedure, eptapirone produces substantial increases in punished responding without affecting unpunished responding, demonstrating marked anxiolytic effects.[1] Furthermore, these effects are more evident than those afforded by buspirone, ipsapirone, and flesinoxan.[1]

Human studies

Eptapirone has been tested in humans in preclinical trials at an oral dose of 1.5 mg.[5][6] In these studies, eptapirone reduces body temperature, suppresses REM sleep, increases cortisol and growth hormone levels, and produces side effects including dizziness and drowsiness while being overall well-tolerated.[5][6] It peaks rapidly within 30-60 minutes and has an estimated half-life of two hours, with a total duration of approximately three hours.[5][6]

See also

References

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GABAA PAMs
Others
α2δ VDCC Blockers
5-HT1A Agonists
Azapirones: Buspirone • Gepirone • Tandospirone; Others: Flesinoxan • Oxaflozane
H1 Antagonists
Diphenylmethanes: Captodiame • Hydroxyzine; Others: Brompheniramine • Chlorpheniramine • Pheniramine
CRH1 Antagonists
NK2 Antagonists
MCH1 antagonists
mGluR2/3 Agonists
mGluR5 NAMs
TSPO agonists
σ1 agonists
Others

M: PSO/PSI

dsrd (o, p, m, p, a, d, s), sysi/epon, spvo

proc, drug(N5A/5B/5C/6A/6B/6D)

Opioids
See also: Opioids template
Opium & alkaloids thereof
Semi-synthetic opium
derivatives
Synthetic opioids
Pyrazolones
Cannabinoids
Anilides
Non-steroidal
anti-inflammatories
See also: NSAIDs template
Propionic acid class
Oxicam class
Acetic acid class
Anthranilic acid
(fenamate) class
Atypical, Adjuvant & Potentiators,
Metabolic agents and miscellaneous
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