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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 high-affinity antagonist of serotonin, norepinephrine, dopamine and histamine receptors, used for the treatment of schizophrenia and acute mania associated with bipolar disorder. ......by AbMole BioScience
Asenapine shows high affinity (pKi) for numerous receptors, including the serotonin 5-HT1A (8.6), 5-HT1B (8.4), 5-HT2A (10.2), 5-HT2B (9.8), 5-HT2C (10.5), 5-HT5A (8.8), 5-HT6 (9.5), and 5-HT7 (9.9) receptors, the adrenergic α1 (8.9), α2A (8.9), α2B (9.5), and α2C (8.9) receptors, the dopamine D1 (8.9), D2 (8.9), D3 (9.4), and D4 (9.0) receptors, and the histamine H1 (9.0) and H2 (8.2) receptors.
......by AdooQ BioScience, LLC
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, also known as Org 5222 and HSDB 8061, is an atypical antipsychotic developed for the treatment of schizophrenia and acute mania associated with bipolar disorder. Preliminary data indicate that it has minimal anticholinergic and cardiovascular side effects, as well as minimal weight gain. FDA approved thisderug in August 2009. ......by MedKoo Biosciences, Inc.
Asenapine maleate (Org 5222) is a potent psychopharmacologic agent that shows high affinity for 5-HT, dopamine, histamine and adrenoceptors; shows much lower affinity (pKi<5) for muscarinic receptor; behaves as a potent antagonist 5-HT receptors (5-HT2A pKB=9.0), dopaime and adrenoceptors; shows strong antipsychotic potential in vivo.SchizophreniaApproved ......by ProbeChem
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
AbMole BioScience USA
AdooQ BioScience, LLC USA
Apexbio Technology LLC USA
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
MedKoo Biosciences, Inc. USA
ProbeChem
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

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More Information

Asenapine (maleate)

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