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Gepirone

CAS No.83928-76-1
Chemical Name:Gepirone
CBNumber:CB11011279
Molecular Formula:C19H29N5O2
Formula Weight:359.47
MOL File:83928-76-1.mol

Gepirone Property

Melting point 106-108°C
Boiling point 562.3±60.0 °C(Predicted)
Density 1.142±0.06 g/cm3 (20 ºC 760 Torr)
storage temp. under inert gas (nitrogen or Argon) at 2-8°C
solubility Chloroform (Slightly), Methanol (Slightly, Heated)
form Solid
pka 7.72±0.10(Predicted)
color Off-White to Pale Yellow
FDA UNII JW5Y7B8Z18
ATC code N06AX19

Hazard and Precautionary Statements (GHS)

Symbol(GHS)
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Gepirone Chemical Properties,Usage,Production

Description Gepirone is a chemical analogue of buspirone and also acts as a partial agonist at 5-HT1A receptors. It is active in animal models predictive of anxiolytic action and also shows antidepressant activity in preclinical studies. With long-term administration, gepirone downregulates 5-HT2 receptors, which is a property common to nearly all antidepressant drugs (Stahl 1994). This dual action, suggesting both anxiolytic and antidepressant effects, is typical of many compounds acting at 5-HT1A receptors and may indicate that such compounds may be useful in the treatment of mixed anxiety and depression (Stahl, in press).
Preliminary phase II clinical data have shown that gepirone is an effective anxiolytic that significantly reduces both psychic and somatic symptoms of generalized anxiety disorder. Like buspirone, gepirone does not impair memory, verbal fluency, or psychomotor performance (Harto and Branconnier 1988).
Uses Gepirone is an antidepressant and anxiolytic of the azapirone class. It acts as a selective partial agonist of the 5-HT1A receptor.
Definition ChEBI: Gepirone is a N-arylpiperazine.

in vivo

Gepirone (0-3 mg/kg for intraperitoneal injection) interacts with progesterone at 5-HT_1A receptors to reduce lordosis behavior in female rats treated with estradiol benzoate and progesterone^[1].
Gepirone (10, 15 mg/kg for subcutaneous injection, 2, 7, or 14 days) activates the normosensitive postsynaptic 5-HT_1A receptor in Male Sprague-Dawley rats^[2].

Animal Model:	Sprague-Dawley rats^[1]
Dosage:	0, 0.1, 0.3, 1 and 3 mg/kg
Administration:	Intraperitoneal injection (i.p.)
Result:	Increases in lordotic activity at lower doses. Inhibited lordosis by the 0.3 and 1.0 mg/kg doses and further inhibition was produced by the 3.0 mg/kg dose.

Animal Model:	Male Sprague-Dawley rats^[2]
Dosage:	10, 15 mg/kg
Administration:	Subcutaneous injection (s.c.)
Result:	Decreased the number of spontaneously active 5-HT neurons and firing rate. Not modified with long-term treatment with ED₅₀ value of 10.1±0.5 μg/kg in controls and 9.7 ±1.9 μg/kg in treated rats.