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Submit ReviewNon-selective 5HT2 antagonist, migraine prophylactic. Also SETD7/9 inhibitor (IC50 = 1μM). Decreases expression and increases degradation of estrogen receptor (ER) α in breast tumor MCF7 cells. Inhibits growth of MCF7 xenografts in mice.
M. Wt | 323.86 |
Formula | C21H21N.HCl |
Storage | Store at RT |
Purity | ≥98% (HPLC) |
CAS Number | 969-33-5 |
PubChem ID | 13770 |
InChI Key | ZPMVNZLARAEGHB-UHFFFAOYSA-N |
Smiles | Cl[H].CN1CC\C(CC1)=C1/C2=C(C=CC=C2)C=CC2=C1C=CC=C2 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
References are publications that support the biological activity of the product.
Hoyer et al (1994) VII. International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (serotonin). Pharmacol.Rev. 46 157 PMID: 7938165
Moran et al (1994) Inhibitory 5-hydroxytryptamine receptors involved in pressor effects obtained by stimulation of sympathetic outflow from spinal cord in pithed rats. Br.J.Pharmacol. 113 1358 PMID: 7889292
Takemoto et al (2016) Identification of cyprohept. as an inhibitor of SET domain containing lysine methyltransferase 7/9 (Set7/9) that regulates estrogen-dependent transcription. J.Med.Chem. 59 3650 PMID: 27088648
Keywords: Cyproheptadine hydrochloride, Cyproheptadine hydrochloride supplier, 5-HT2, antagonists, Non-Selective, Serotonin, Receptors, antagonism, inhibitors, inhibits, lysine, methyltransferase, SETD7/9, epigenetics, Non-selective, Other, Lysine, Methyltransferases, 0996, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for Cyproheptadine hydrochloride include:
Fouad et al (2010) Locomotion after spinal cord injury depends on constitutive activity in serotonin receptors. J Neurophysiol 104 2975 PMID: 20861436
Murray et al (2010) Recovery of motoneuron and locomotor function after spinal cord injury depends on constitutive activity in 5-HT2C receptors. Nat Med 16 694 PMID: 20512126
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.