Asenapine maleate(Org 5222 maleate)

Molecular Weight (MW)	401.84
Formula	C17H16ClNO.C4H4O4
CAS No.	85650-56-2
Storage	-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)	DMSO: 80 mg/mL (199.1 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Other info	Chemical Name: (3aS,12bS)-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenzo[2,3:6,7]oxepino[4,5-c]pyrrole maleate InChi Key: GMDCDXMAFMEDAG-CHHFXETESA-N InChi Code: InChI=1S/C17H16ClNO.C4H4O4/c1-19-9-14-12-4-2-3-5-16(12)20-17-7-6-11(18)8-13(17)15(14)10-19;5-3(6)1-2-4(7)8/h2-8,14-15H,9-10H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1-/t14-,15-;/m1./s1 SMILES Code: CN1C[C@@](C2=CC=CC=C2OC3=CC=C(Cl)C=C34)([H])[C@]4([H])C1.O=C(O)/C=C\C(O)=O
Synonyms	Org 5222; HSDB 8061; Org 5222; HSDB 8061; Org5222; Org-5222; HSDB-8061; HSDB8061; Asenapine; Asenapine maleate; trade names Saphris and Sycrest.

Molecular Weight (MW)

401.84

Formula

C17H16ClNO.C4H4O4

CAS No.

85650-56-2

Storage

-20℃ for 3 years in powder form

-80℃ for 2 years in solvent

Solubility (In vitro)

DMSO: 80 mg/mL (199.1 mM)

Water: <1 mg/mL

Ethanol: <1 mg/mL

Other info

Chemical Name: (3aS,12bS)-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenzo[2,3:6,7]oxepino[4,5-c]pyrrole maleate

InChi Key: GMDCDXMAFMEDAG-CHHFXETESA-N

InChi Code: InChI=1S/C17H16ClNO.C4H4O4/c1-19-9-14-12-4-2-3-5-16(12)20-17-7-6-11(18)8-13(17)15(14)10-19;5-3(6)1-2-4(7)8/h2-8,14-15H,9-10H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1-/t14-,15-;/m1./s1

SMILES Code: CN1C[C@@](C2=CC=CC=C2OC3=CC=C(Cl)C=C34)([H])[C@]4([H])C1.O=C(O)/C=C\C(O)=O

Synonyms

Org 5222; HSDB 8061; Org 5222; HSDB 8061; Org5222; Org-5222; HSDB-8061; HSDB8061; Asenapine; Asenapine maleate; trade names Saphris and Sycrest.

In Vitro	In vitro activity: Asenapine shows high affinity and a different rank order of binding affinities (pKi) for serotonin receptors (5-HT1A [8.6], 5-HT1B [8.4], 5-HT2A [10.2], 5-HT2B [9.8], 5-HT2C [10.5], 5-HT5 [8.8], 5-HT6 [9.6] and 5-HT7 [9.9]), adrenoceptors (alpha1 [8.9], alpha2A [8.9], alpha2B [9.5] and alpha2C [8.9]), dopamine receptors (D1 [8.9], D2 [8.9], D3 [9.4] and D4 [9.0]) and histamine receptors (H1 [9.0] and H2 [8.2]). Asenapine has a higher affinity for 5-HT2C, 5-HT2A, 5-HT2B, 5-HT7, 5-HT6, alpha2B and D3 receptors, suggesting stronger engagement of these targets at therapeutic doses. Asenapine behaves as a potent antagonist (pKB) at 5-HT1A (7.4), 5-HT1B (8.1), 5-HT2A (9.0), 5-HT2B (9.3), 5-HT2C (9.0), 5-HT6 (8.0), 5-HT7 (8.5), D2 (9.1), D3 (9.1), alpha2A (7.3), alpha2B (8.3), alpha2C (6.8) and H1 (8.4) receptors. Kinase Assay: Relative to its D2 receptor affinity, asenapine has a higher affinity for 5-HT2C, 5-HT2A, 5-HT2B, 5-HT7, 5-HT6, α2B and D3 receptors, suggesting stronger engagement of these targets at therapeutic doses. Asenapine behaves as a potent antagonist (pKB) at 5-HT1A (7.4), 5-HT1B (8.1), 5-HT2A (9.0), 5-HT2B (9.3), 5-HT2C (9.0), 5-HT6 (8.0), 5-HT7 (8.5), D2 (9.1), D3 (9.1), α2A (7.3), α2B (8.3), α2C (6.8) and H1 (8.4) receptors.
In Vivo	Asenapine is an atypical antipsychotic that is currently available for the treatment of schizophrenia and bipolar I disorder. Asenapine may have superior therapeutic effect on anxiety symptoms than other agents in rats. Asenapine has anxiolytic-like effects in the EPM and the defensive marble burying tests in mice.
Animal model	Rats: Asenapine maleate is suspended in 10% hydroxypropyl-β-cyclodextrin and administered in a volume of 1 mL/kg body weight . Rats are individually fear conditioned using electrical foot shock in a Skinner box. Animals are injected intraperitoneally (i.p.) with asenapine, clozapine, olanzapine, buspirone, or SB242084 at 30 min before freezing behaviour assessment. Mice: Male ICR mice are repeatedly treated with 0.1 or 0.3mg/kg injections of asenapine and then tested in a battery of behavioural tests related to anxiety including the open-field test, elevated plus-maze (EPM), defensive marble burying and hyponeophagia tests.
Formulation & Dosage	Mice: 0.1 or 0.3mg/kg; Rats: 1 mL/kg, injections
References	J Psychopharmacol. 2009 Jan;23(1):65-73; Psychopharmacology (Berl). 2008 Feb;196(3):417-29.

In Vitro

In vitro activity: Asenapine shows high affinity and a different rank order of binding affinities (pKi) for serotonin receptors (5-HT1A [8.6], 5-HT1B [8.4], 5-HT2A [10.2], 5-HT2B [9.8], 5-HT2C [10.5], 5-HT5 [8.8], 5-HT6 [9.6] and 5-HT7 [9.9]), adrenoceptors (alpha1 [8.9], alpha2A [8.9], alpha2B [9.5] and alpha2C [8.9]), dopamine receptors (D1 [8.9], D2 [8.9], D3 [9.4] and D4 [9.0]) and histamine receptors (H1 [9.0] and H2 [8.2]). Asenapine has a higher affinity for 5-HT2C, 5-HT2A, 5-HT2B, 5-HT7, 5-HT6, alpha2B and D3 receptors, suggesting stronger engagement of these targets at therapeutic doses. Asenapine behaves as a potent antagonist (pKB) at 5-HT1A (7.4), 5-HT1B (8.1), 5-HT2A (9.0), 5-HT2B (9.3), 5-HT2C (9.0), 5-HT6 (8.0), 5-HT7 (8.5), D2 (9.1), D3 (9.1), alpha2A (7.3), alpha2B (8.3), alpha2C (6.8) and H1 (8.4) receptors.

Kinase Assay: Relative to its D2 receptor affinity, asenapine has a higher affinity for 5-HT2C, 5-HT2A, 5-HT2B, 5-HT7, 5-HT6, α2B and D3 receptors, suggesting stronger engagement of these targets at therapeutic doses. Asenapine behaves as a potent antagonist (pKB) at 5-HT1A (7.4), 5-HT1B (8.1), 5-HT2A (9.0), 5-HT2B (9.3), 5-HT2C (9.0), 5-HT6 (8.0), 5-HT7 (8.5), D2 (9.1), D3 (9.1), α2A (7.3), α2B (8.3), α2C (6.8) and H1 (8.4) receptors.

In Vivo

Asenapine is an atypical antipsychotic that is currently available for the treatment of schizophrenia and bipolar I disorder. Asenapine may have superior therapeutic effect on anxiety symptoms than other agents in rats. Asenapine has anxiolytic-like effects in the EPM and the defensive marble burying tests in mice.

Animal model

Rats: Asenapine maleate is suspended in 10% hydroxypropyl-β-cyclodextrin and administered in a volume of 1 mL/kg body weight . Rats are individually fear conditioned using electrical foot shock in a Skinner box. Animals are injected intraperitoneally (i.p.) with asenapine, clozapine, olanzapine, buspirone, or SB242084 at 30 min before freezing behaviour assessment.

Mice: Male ICR mice are repeatedly treated with 0.1 or 0.3mg/kg injections of asenapine and then tested in a battery of behavioural tests related to anxiety including the open-field test, elevated plus-maze (EPM), defensive marble burying and hyponeophagia tests.

Formulation & Dosage

Mice: 0.1 or 0.3mg/kg; Rats: 1 mL/kg, injections

References

J Psychopharmacol. 2009 Jan;23(1):65-73; Psychopharmacology (Berl). 2008 Feb;196(3):417-29.

CAS NO:	85650-56-2
规格:	≥98%

包装	价格(元)
25mg	电议
50mg	电议
100mg	电议
250mg	电议
500mg	电议
1g	电议
2g	电议
5g	电议