Cat. No. 0996
Chemical Name: 4-(5H-Dibenzo[a,d]cyclohepten-5-yli
Biological ActivityNon-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.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Safety Data Sheet
Takemoto et al (2016) Identification of cyproheptadine 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.
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.
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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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Keywords: Cyproheptadine hydrochloride, supplier, 5-HT2, antagonists, Non-Selective, Serotonin, Receptors, antagonism, inhibitors, inhibits, lysine, methyltransferase, SETD7/9, epigenetics, Tocris Bioscience, Non-selective 5-HT2 Antagonist products
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