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85650-56-2 (Asenapine (maleate))

1

Identification

Asenapine (maleate) Asenapine (maleate)
Name Asenapine (maleate)
Formula C21H20ClNO5
MW 401.84
CAS No. 85650-56-2
EINECS 288-064-8
Smiles CN1C[[email protected]]2([H])C3=CC=CC=C3OC4=CC=C(Cl)C=C4[[email protected]]2(C1)[H].O=C(O)/C=CC(O)=O
Synonyms Saphris maleate;Org 5222 maleate;Org-5222 maleate;Org5222 maleate; (3aS,12bS)-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenzo[2,3:6,7]oxepino[4,5-c]pyrrole maleate
InChI 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
2

Introduction

Asenapine maleate(Org 5222 maleate) inhibits adrenergic receptor (α1, α2A, α2B, α2C) with Ki of 0.25-1.2 nM and also inhibits 5-HT receptor (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) with Ki of 0.03-4.0 nM.

Background Information

Asenapine Maleate is a 5-HT receptor antagonist used for the treatment of acute schizophrenia and bipolar mania. It is a second-generation (atypical) antipsychotic agent. ......by BOC Sciences
Asenapine maleate is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and D2 angonist with Ki values of 0.03-4.0 nM, 1.3nM,respectively, and an antipsychotic. ......by MedChemexpress Co., Ltd.
Asenapine maleate is a high-affinity antagonist of serotonin, norepinephrine, dopamine and histamine receptors, used for the treatment of schizophrenia and acute mania associated with bipolar disorder. ......by Selleck Chemicals LLC
Developed by Schering-Plough after its merger with Organon International, asenapine is a sublingually administered, atypical antipsychotic for treatment of schizophrenia and acute mania associated with bipolar disorder. Asenapine also belongs to the dibenzo-oxepino pyrrole class. It is also for severe post-traumatic stress disorder nightmares in soldiers as an off-label use. FDA approved on August 13, 2009. ......by Target Molecule Corp.
Novel psychopharmacologic agent. Displays antagonist activity at 5-HT, dopamine, noradrenalin and histamine receptor subtypes (pKi values are 8.60, 8.40, 10.15, 9.75, 10.46, 8.84, 9.60, 9.94, 8.85, 8.90, 8.84, 9.38, 8.95, 8.93, 8.9, 9.49, 8.91, 9.00 and 8.21 for 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT5A, 5-HT6, 5-HT7, D1, D2L, D2S, D3, D4, α1A, α2A, α2B, α2C, H1 and H2 receptors respectively). Displays no appreciable affinity for muscarinic receptors. Exhibits potent activity in animal models predictive of antipsychotic efficacy. ......by Tocris Bioscience Inc.
3

Protocol(Only for Reference)

Cell Experiment

Animal Experiment

4

Physical and Chemical Properties

Appearance:White to off-white Solid EBNumber:EB000023713

Storage condition

Store at +4°C by Tocris Bioscience Inc.

Solubility

DMSO >80 mg/mL Ethanol >12 mg/mL by MedChemexpress Co., Ltd.
(25°C) * In vitro DMSO 80 mg/mL (199.08 mM); Water<1 mg/mL (<1 mM); Ethanol<1 mg/mL (<1 mM) by Selleck Chemicals LLC
Soluble to 100 mM in DMSO and to 50 mM in ethanol by Tocris Bioscience Inc.
5

Mechanism and Indication

6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
Asenapine (maleate) Centre de recherche de l'Institut universitaire en santé mentale de Québec Schizophrenia 2013/10/31 2014/3/31 Phase 4 Clinical
Asenapine (maleate) University of California Irvine Stutter 2012/9/30 2013/12/31 Phase 4 Clinical
Asenapine (maleate) Duke University Depression 2012/10/31 2014/2/28 Phase 4 Clinical
Asenapine (maleate) Tuscaloosa Research and Education Advancement Corporation Post traumatic stress disorder 2012/6/30 2013/8/31 Phase 4 Clinical
Asenapine (maleate) Duke University Schizophrenia 2012/3/31 2013/7/31 Phase 4 Clinical
Asenapine (maleate) Centre de recherche de l'Institut universitaire en santé mentale de Québec Psychotic disorder 2013/10/31 2014/3/31 Phase 4 Clinical
Asenapine (maleate) - Launched
7

Safety Data of Asenapine (maleate)

Hazard Symbols : Xn,N,T,F
Risk Statements : 22-36/37/38-50/53-39/23/24/25-23/24/25-11
Safety Statements : 26-60-61-45-36/37-16
8

Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
BOC Sciences 1g/USD175(In stock)
Beijing Eagle Sky Pharmatech Co., Ltd. China
Beijing Lang Rebone Technology Co., Ltd. China
Biochempartner Co., Ltd China
CHEMSCENE, LLC 10mg/USD60();50mg/USD120() USA
Datang (Hangzhou) Pharmachem Co., Ltd. China
MedChemexpress Co., Ltd. 10mg/USD60();50mg/USD120() USA
Selleck Chemicals LLC 10mg/USD50(In stock);10mM/1mLIn DMSO/USD70(In stock);50mg/USD170(In stock);100mg/USD270(In stock) USA
Shanghai Everchem Co., Ltd. China
Shanghai Growingchem Co., Ltd. China
Shanghai Haoyuan Chemexpress Co., Ltd. 10mg/USD60();50mg/USD120() China
Target Molecule Corp. 2mg/USD59();10mg/USD89();50mg/USD168();100mg/USD298() USA
Tocris Bioscience Inc. USA
10

Related Products

Other Forms of 85650-56-2

Name CAS No Formula MW
Asenapine (hydrochloride) 1412458-61-7 C17H17Cl2NO 322.23
Asenapine 65576-45-6 C17H16ClNO 285.77

Recommended Compounds in Adrenergic Receptor 5-HT Receptor

Name CAS No Formula MW
Tolazoline 59-98-3 C10H12N2 160.22
Synephrine (hydrochloride) 5985-28-4 C9H14ClNO2 203.67
(R)-(-)-Phenylephrine 59-42-7 C9H13NO2 167.205
Nicergoline 27848-84-6 C24H26BrN3O3 484.39
Tamsulosin (hydrochloride) 106463-17-6 C20H29ClN2O5S 444.97
Tamsulosin 106133-20-4 C20H28N2O5S 408.51
UK 14,304 59803-98-4 C11H10BrN5 292.13
Guanfacine 29110-47-2 C9H9Cl2N3O 246.09
Propranolol (hydrochloride) 318-98-9 C16H22ClNO2 295.8
Guanabenz (Acetate) 23256-50-0 C10H12Cl2N4O2 291.13
Tetrahydrozoline (hydrochloride) 522-48-5 C13H17ClN2 236.74
Octopamine (hydrochloride) 770-05-8 C8H12ClNO2 189.64
Betaxolol (hydrochloride) 63659-19-8 C18H30ClNO3 343.89
Indacaterol (maleate) 753498-25-8 C28H32N2O7 508.56
Medetomidine (hydrochloride) 86347-15-1 C13H17ClN2 236.74
Norepinephrine (bitartrate monohydrate) 108341-18-0 C12H19NO10 337.28
Norepinephrine (hydrochloride) 329-56-6 C8H12ClNO3 205.64
Xylometazoline (hydrochloride) 1218-35-5 C16H25ClN2 280.84
(R)-(-)-Phenylephrine (hydrochloride) 61-76-7 C9H14ClNO2 203.67
Isoprenaline (hydrochloride) 51-30-9 C11H18ClNO3 247.72

Recommended Compounds in Same Indication

Name CAS No Formula MW
Iloperidone 133454-47-4 C24H27FN2O4 426.48
Rifabutin 72559-06-9 C46H62N4O11 847.0
Tianeptine 72797-41-2 C21H25ClN2O4S 436.95
Cariprazine 839712-12-8 C21H32Cl2N4O 427.41
PF-2545920 898562-94-2 C25H20N4O 392.45
lumateperone (Tosylate) 1187020-80-9 C31H36FN3O4S 565.6987
Lu AE58054 467459-31-0 C20H19F5N2O 398.37
EVP-6124 550999-75-2 C16H17ClN2OS 320.84
Asenapine 65576-45-6 C17H16ClNO 285.77
Adoprazine 222551-17-9 C24H24FN3O2 405.46
Vortioxetine 508233-74-7 C18H22N2S 298.45
Clozapine 5786-21-0 C18H19ClN4 326.82
Rolipram 61413-54-5 C16H21NO3 275.34
Nepicastat (hydrochloride) 170151-24-3 C14H16ClF2N3S 331.8117
Mifepristone 84371-65-3 C29H35NO2 429.59
Bitopertin 845614-11-1 C21H20F7N3O4S 543.46
Bitopertin (R enantiomer) 845614-12-2 C21H20F7N3O4S 543.46
Zolpidem 82626-48-0 C19H21N3O 307.39
Lurasidone (Hydrochloride) 367514-88-3 C28H37ClN4O2S 529.14
Preladenant 377727-87-2 C25H29N9O3 503.56
11

Route of Synthesis

12

References

13

More Information

Asenapine (maleate)

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