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Chemical Structure| 74050-98-9 Chemical Structure| 74050-98-9

Structure of Ketanserin
CAS No.: 74050-98-9

Chemical Structure| 74050-98-9

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Ketanserin is a specific 5-HT2A serotonin receptor antagonist with Ki of 2.5 nM for rat and human 5-HT2A, used as an antihypertensive drug.

Synonyms: R41468; Ketanserinum

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Product Details of Ketanserin

CAS No. :74050-98-9
Formula : C22H22FN3O3
M.W : 395.43
SMILES Code : FC1=CC=C(C=C1)C(C2CCN(CC2)CCN3C(NC4=CC=CC=C4C3=O)=O)=O
Synonyms :
R41468; Ketanserinum
MDL No. :MFCD00083392
InChI Key :FPCCSQOGAWCVBH-UHFFFAOYSA-N
Pubchem ID :3822

Safety of Ketanserin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Ketanserin

GPCR

Isoform Comparison

Biological Activity

Target
  • 5-HT2

    5-HT2C (Human), Ki:2.5 nM

    5-HT2C (Rat), Ki:50 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Bone-marrow-derived macrophages (BMDMs) 10^-9 M 2 days Macrophages conditioned with Ketanserin showed a lower pro-fibrotic phenotype in a co-culture system with mesenchymal cells and reduced Col1a1 expression. PMC6053408
Spleen cells 25 nM Ketanserin, a specific antagonist of the 5-HT2A receptor, significantly reduced the number of osteoclasts in WT spleen cell cultures. PMC3289318
18-81 pre-B cell line 1-10 μM 10-15 min Ketanserin, a specific antagonist of 5-HT2 receptors, was used to study the effects of 5-HT on potassium currents. Results showed that Ketanserin had no significant effect on 5-HT-induced changes in current amplitude or inactivation rate, indicating that 5-HT2 receptors are not involved in the modulation. PMC280470

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice SERTKO and wild-type mice Intraperitoneal injection 1 mg/kg/day Daily for 5 days Ketanserin almost eliminated apoptosis in SERTKO mice and significantly reduced villus height, crypt depth, and crypt proliferation index. PMC3687781
Mice Genetically mast cell-deficient mouse model In vitro administration 10^-5 M At least 15 minutes In normal mice, ketanserin significantly inhibited the first phase of the antigen-induced Isc response, but had no significant effect in mast cell-deficient mice. PMC296360
C57BL/6 mice 30% TBSA thermal injury model Intraperitoneal injection 10 mg/kg Daily administration for 21 days (7 days pre-injury and 14 days post-injury) Ketanserin reduced portal fibrosis in thermally injured mice by modulating the phenotype of macrophages away from their pro-fibrotic state. PMC6053408
Mice Chronic multimodal stress model Intraperitoneal injection 2 mg/kg Single injection, 60 minutes before psilocybin administration To test whether ketanserin could block the antidepressant-like behavioral responses to psilocybin. Results showed that ketanserin pretreatment did not prevent the anti-anhedonic effects of psilocybin. PMC8092378
Mice Maternal immune activation (MIA) model Intraperitoneal injection 2 mg/kg Daily for 7 days Chronic ketanserin treatment reduces DOI-induced head twitching in MIA offspring PMC4066472

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.53mL

0.51mL

0.25mL

12.64mL

2.53mL

1.26mL

25.29mL

5.06mL

2.53mL

References

 

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