1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor
  3. Lerimazoline

Lerimazoline is a selective 5-HT1D receptor agonist with Ki values of 72 and 3480 nM for h5-HT1D and h5-HT1B. Lerimazoline inhibits Forskolin (HY-15371)-stimulated cAMP production and induces contractions in rabbit saphenous vein preparations. Lerimazoline can be used for the research of migraine.

For research use only. We do not sell to patients.

Lerimazoline

Lerimazoline Chemical Structure

CAS No. : 54765-26-3

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Description

Lerimazoline is a selective 5-HT1D receptor agonist with Ki values of 72 and 3480 nM for h5-HT1D and h5-HT1B. Lerimazoline inhibits Forskolin (HY-15371)-stimulated cAMP production and induces contractions in rabbit saphenous vein preparations. Lerimazoline can be used for the research of migraine[1].

IC50 & Target[1]

5-HT1D Receptor

72 nM (Ki)

5-HT1B Receptor

3480 nM (Ki)

In Vitro

Lerimazoline (Compound 29) (0.1-1 μM; 60 min) binds to human h5-HT1B receptors with a Ki of 3480 nM[1].
Lerimazoline (0.1-1 μM; 60 min) binds to human h5-HT1D receptors with a Ki of 72 nM, displaying 48-fold selectivity for h5-HT1D over h5-HT1B receptors[1].
Lerimazoline (1-10 μM; 30 min) inhibits Forskolin (HY-15371)-stimulated cAMP production in transfected CHO Pro 5 cells[1].
Lerimazoline (10-10000 nM) induces contractions of rabbit saphenous vein with a 95% of the maximal effect[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

202.30

Formula

C13H18N2

CAS No.
SMILES

CC1=C(CC2=NCCN2)C(C)=CC(C)=C1

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Lerimazoline
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HY-135079
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