| CAS |
41354-29-4 |
| Chinese Name |
盐酸赛庚啶倍半水合物 |
| English Name |
Cyproheptadine Hydrochloride Sesquihydrate |
| Synonyms |
Periactin hydrochloride;Peritol;Cyproheptadine hydrochloride sesquihydrate;盐酸赛庚啶半水合物 |
| Molecular Formula |
C21H21N·3/2H2O·HCl |
| Molecular Weight |
350.88 |
| Solubility |
Soluble in DMSO ≥3mg/mL |
| Purity |
≥98% |
| Appearance |
White to off-white Solid |
| Storage |
Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC |
EINECS 213-535-1 |
| MDL |
MFCD00012538 |
| SMILES |
CN1CCC(=C2C3=CC=CC=C3C=CC4=CC=CC=C42)CC1.CN1CCC(=C2C3=CC=CC=C3C=CC4=CC=CC=C42)CC1.O.O.O.Cl.Cl |
| InChIKey |
ZEAUHIZSRUAMQG-UHFFFAOYSA-N |
| InChI |
InChI=1S/2C21H21N.2ClH.3H2O/c2*1-22-14-12-18(13-15-22)21-19-8-4-2-6-16(19)10-11-17-7-3-5-9-20(17)21;;;;;/h2*2-11H，12-15H2，1H3;2*1H;3*1H2 |
| PubChem CID |
11954233 |
| Target Point |
5-HT Receptor;SETD7/9 |
| Passage |
Neuronal Signaling；GPCR & G Protein;Epigenetics |
| Background |
It is a non-selective 5HT2 antagonist; It is also an inhibitor of SETD7/9. |
| Biological Activity |
Cyproheptadine Hydrochloride 是一种非选择性的 5HT2 受体拮抗剂，其IC50为0.6 nM，也是一种 SETD7/9 抑制剂。[1-3] |
| IC50 |
5-HT2: 0.6nM(IC50)[1];SETD7/9: 1μM(IC50)[3] |
| In Vitro |
Subthreshold concentration of 5-HT(2 micromol/L)potentiated the effect of low dose of arachidonic acid(AA)(0.2 mmol/L)in human platelets. This synergistic effect was blocked by 5-HT2 receptor antagonist(cyproheptadine IC(50)=0.6 nmol/L).[1] Cyproheptadine binds in the substrate-binding pocket of Set7/9 and inhibits its enzymatic activity by competing with the methyl group acceptor. Treatment of human breast cancer cells(MCF7 cells)with cyproheptadine decreased the expression and transcriptional activity of ERα，thereby inhibiting estrogen-dependent cell growth.[3] |
| In Vivo |
Cyproheptadine significantly inhibited facilitatory effects of 1-(2，5-dimethoxy-4-iodophenyl)-2-aminopropane(DOI)on flexor reflexes and mono- and polysynaptic spinal reflex potentials in spinalized rats.[2] |
| Cell Experiment |
Treatment of human breast cancer cells(MCF7 cells)with cyproheptadine decreased the expression and transcriptional activity of ERα，thereby inhibiting estrogen-dependent cell growth. [3] |
| Kinase Experiment |
Kinetic and X-ray crystallographic analyses revealed that cyproheptadine binds in the substrate-binding pocket of Set7/9 and inhibits its enzymatic activity by competing with the methyl group acceptor. [3] |
| Data Literature Source |
[1]. Saeed SA，et al. Synergism interaction between arachidonic acid by 5-hydroxytryptamine in human platelet aggregation is mediated through multiple signalling pathways. Acta Pharmacol Sin. 2003 Oct;24(10):958-64.
[2]. Honda M，et al. Tricyclic analogs cyclobenzaprine，amitriptyline and cyproheptadine inhibit the spinal reflex transmission through 5-HT(2) receptors. Eur J Pharmacol. 2003 Jan 1;458(1-2):91-9.
[3]. Takemoto Y，et al. Identification of Cyproheptadine as an Inhibitor of SET Domain Containing Lysine Methyltransferase 7/9 (Set7/9) That Regulates Estrogen-Dependent Transcription. J Med Chem. 2016 Apr 28;59(8):3650-60. |
| Unit |
Bottle |
| Specification |
25mg 50mg |
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