Home Neuronal Signaling 5-HT Receptor inhibitor - Dopamine Receptor inhibitor - Adrenergic Receptor inhibitor - Histamine Receptor inhibitor - AChR inhibitor Pimethixene maleate For research use only.

Pimethixene maleate

Synonyms: Pimetixene maleate

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.

Pimethixene maleate Chemical Structure

Pimethixene maleate Chemical Structure

CAS: 13187-06-9

Purity & Quality Control

Batch: S391301 DMSO] 82 mg/mL] false] Ethanol] 7 mg/mL] false] Water] Insoluble] false Purity: 99.97%
99.97

Pimethixene maleate Related Products

Signaling Pathway

5-HT Receptor Signaling Pathways

5-HT Receptor Signaling Pathway

Choose Selective 5-HT Receptor Inhibitors

Biological Activity

Description 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.
Targets
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)		 Click to View More Targets
10.44(pKi) 10.22(pKi) 10.14(pKi) 9.38(pKi) 8.61(pKi)
In vitro
In vitro

Pimethixene shows the least potency against pancreatic cancer cell lines with an IC50 up to a millimolar concentration.[2]
Cell Research Cell lines pancreatic cancer cell lines
Concentrations 10 pM-5 mM
Incubation Time 4 days
Method

For IC50 determination of drugs, 5000 cells were seeded in 96‐well plates on day 0. On day 1, drugs in a series of 10‐fold dilutions were added to the cells. For dasatinib and FTY‐720, the doses were from 10 μM to 10 pM; For phenothiazines, the concentration was from 100 μM except pimethixene (5 mM). On day 4, MTT (3‐(4,5‐Dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide) based assays were performed and absorbance was measured at 595 nm with 630 nm.

Chemical Information & Solubility

Molecular Weight 409.5 Formula

C23H23NO4S
CAS No. 13187-06-9 SDF --
Smiles CN1CCC(CC1)=C2C3=CC=CC=C3SC4=CC=CC=C24.OC(=O)\C=C/C(O)=O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 82 mg/mL ( (200.24 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 7 mg/mL

Water : Insoluble


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In vivo
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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