Pimethixene maleate
Cat. No.: DC44781
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Chemical Structure
13187-06-9
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Field of application
Pimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7.30, 7.28, 7.61, 6.37, 8.19, 7.54, 10.14, 8.61 and 9.38, respectively.,5-HT2B [1](Cell-free assay)
5-HT2A [1](Cell-free assay)
Histamine H1 Receptor [1](Cell-free assay)
Muscarinic M2 [1](Cell-free assay)
Muscarinic M1 [1](Cell-free assay)
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10.44(pKi)
10.22(pKi)
10.14(pKi)
9.38(pKi)
8.61(pKi)
Cas No.: |
13187-06-9 |
Chemical Name: |
9-(1-Methyl-4-piperidylene)thioxanthene maleate |
Synonyms: |
9-(1-Methyl-4-piperidylene)thioxanthene maleate;1-METHYL-4-[THIOXANTHEN-9-YLIDENE]PIPERIDINE MALEATE SALT;PIMETHIXEN MALEATE SALT;Pimethixene maleate salt;1-methyl-4-(9H-thioxanthen-9-ylidene)piperidinium hydrogen maleate;1-Methyl-4-(thioxanthen-9-ylidene)piperidine;9-(1-methyl-4-piperidylene)-thioxanthenmaleate;9-(n-methyl-piperidyliden-4)thioxanemaleate;bp-400;PIMETHIXENE MALEATE;Pimethixene maleic salt;PIMETHIXENE MALEATE SALT;9-(1-methyl-4-piperidylene)thioxanthenemaleate |
SMILES: |
OC(/C=C/C(=O)O)=O.CN1CC/C(=C2/C3=CC=CC=C3SC3=CC=CC=C/23)/CC1 |
Formula: |
C23H23NO4S |
M.Wt: |
409.498025178909 |
Purity: |
>98% |
Sotrage: |
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: |
Pimethixene maleate is antihistamine and antiserotonergic compound, acts as an antimigraine agent.Pimethixene maleate is a highly potent antagonist of 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors, with pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively[1]. |
Target: |
pKi: 7.63 (5-HT1A receptor), 10.22 (5-HT2A receptor), 10.44 (5-HT2B receptor), 8.42 (5-HT2C receptor), 10.14 (histamine H1 receptor), 8.19 (D2 receptor), 7.54 (DD4.4 receptor), 8.61 (M1 receptor), 9.38 (M2 receptor)[1] |
References: |
[1]. Schmitz B, et al. BF-1--a novel selective 5-HT2B receptor antagonist blocking neurogenic dural plasma protein extravasation in guinea pigs. Eur J Pharmacol. 2015 Mar 15;751:73-80. |
MSDS
COA
LOT NO. |
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2018-0101 |
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