| Identification | Back Directory | [Name]
2-[4-[4-(2-PYRIMIDINYL)-1-PIPERAZINYL]BUTYL]-1,2-BENZISOTHIAZOL-3(2H)-ONE-1,1-DIOXIDE | [CAS]
95847-70-4 | [Synonyms]
Isapirone
IPSAPIRONE
1,2-benzisothiazol-3(2h)-one,2-(4-(4-(2-pyrimidinyl)-1-piperazinyl)butyl)-,1,
2-[4-[4-(2-PYRIMIDINYL)-1-PIPERAZINYL]BUTYL]-1,2-BENZISOTHIAZOL-3(2H)-ONE-1,1-DIOXIDE
2-(4-(4-(Pyrimidin-2-yl)piperazin-1-yl)butyl)benzo[d]isothiazol-3(2H)-one 1,1-dioxide | [Molecular Formula]
C19H23N5O3S | [MDL Number]
MFCD00866976 | [MOL File]
95847-70-4.mol | [Molecular Weight]
401.48 |
| Chemical Properties | Back Directory | [Melting point ]
137-138° | [Boiling point ]
629.8±65.0 °C(Predicted) | [density ]
1.345±0.06 g/cm3(Predicted) | [storage temp. ]
Store at RT | [solubility ]
Soluble to 10 mM in DMSO | [form ]
Powder | [pka]
7.69±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Anti-anxiety agent
. | [Definition]
ChEBI: 1,1-dioxo-2-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-1,2-benzothiazol-3-one is a N-arylpiperazine. | [Biological Activity]
Selective 5-HT 1A receptor agonist (K i = 10 nM). Anxiolytic in vivo . | [in vivo]
Ipsapirone inhibits induced by 8-OH-DPAT and 5-methoxydimethyltryptamine (agonists of 5-HT1A receptors) behavioural effects (flat body posture and forepaw treading) in normal and reserpinized rats[1].
Ipsapirone (2.5-80 mg/kg), given alone to rats induces a slight flattening of body posture (~ 1 point at the highest dose) and a mild hind limb abduction observed at doses 2.5-80 mg/kg. Ipsapirone given alone at low doses (2.5-10 mg/kg i.p.) does not significantly change the body temperature in rats and mice, but decreased it in both those species at high doses (35 mg/kg i.p.) by ca. 2-2.5℃[1].
| Animal Model: | Male Albino-Swiss mice (18-24 g) and male Wistar rats (160-200 g)[1].
| | Dosage: | 5 and 10 mg/kg. | | Administration: | IP 30 min before 8-OH-DPAT and 5-MeODMT injections. | | Result: | Behavioural responses (flat body posture, forepaw treading) to 8-OH-DPAT (5 mg/kg s.c.) in rats were antagonized by Ipsapirone (5 and 10 mg/kg i.p.). |
| [IC 50]
5-HT1A Receptor | [storage]
Store at RT |
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