HT-0712

Chemical compound

None

Identifiers

IUPAC name

(3S,5S)-5-(3-(Cyclopentyloxy)-4-methoxyphenyl)-3-(3-methylbenzyl)piperidin-2-one

CAS Number

617720-02-2

PubChem CID

9865375

ChemSpider

8041067^Y

UNII

2O43FXG9IG

CompTox Dashboard (EPA)

DTXSID70893926

Chemical and physical dataFormulaC₂₅H₃₁NO₃Molar mass393.527 g·mol⁻¹3D model (JSmol)

Interactive image

SMILES

O=C3NC[C@H](c2cc(OC1CCCC1)c(OC)cc2)C[C@H]3Cc4cccc(c4)C

InChI

InChI=1S/C25H31NO3/c1-17-6-5-7-18(12-17)13-20-14-21(16-26-25(20)27)19-10-11-23(28-2)24(15-19)29-22-8-3-4-9-22/h5-7,10-12,15,20-22H,3-4,8-9,13-14,16H2,1-2H3,(H,26,27)/t20-,21-/m1/s1^Y
Key:ABEJDMOBAFLQNJ-NHCUHLMSSA-N^Y

(verify)

HT-0712, also known as IPL-455903,^[1] is an experimental cognitive enhancing drug (nootropic) which is currently undergoing clinical trials. It is currently being licensed by Helicon Therapeutics in San Diego, California. It was originally discovered and tested as part of a preclinical anti-inflammatory program by Inflazyme Pharmaceuticals.^[2]

Mechanism of action

HT-0712 appears to act as a PDE4 inhibitor, thereby increasing cAMP levels. When cAMP levels are increased in neurons, this may trigger the activation of cAMP response element-binding proteins (CREB). CREBs are transcription factors involved in the formation of long-term memory.^[2]

The side effects of the drug are not yet fully known.

Research

A 2014 study found that HT-0712 significantly boosted memory formation in mice. Data also indicated that HT-0712 may be effective to treat age-associated memory impairment in humans.^[3]

References

^ Giembycz MA (October 2008). "Can the anti-inflammatory potential of PDE4 inhibitors be realized: guarded optimism or wishful thinking?". British Journal of Pharmacology. 155 (3): 288–290. doi:10.1038/bjp.2008.297. PMC 2567889. PMID 18660832.
^ ^a ^b MacDonald E, Van der Lee H, Pocock D, Cole C, Thomas N, VandenBerg PM, et al. (2007). "A novel phosphodiesterase type 4 inhibitor, HT-0712, enhances rehabilitation-dependent motor recovery and cortical reorganization after focal cortical ischemia". Neurorehabilitation and Neural Repair. 21 (6): 486–496. doi:10.1177/1545968307305521. PMID 17823313.
^ Peters M, Bletsch M, Stanley J, Wheeler D, Scott R, Tully T (December 2014). "The PDE4 inhibitor HT-0712 improves hippocampus-dependent memory in aged mice". Neuropsychopharmacology. 39 (13): 2938–2948. doi:10.1038/npp.2014.154. PMC 4229572. PMID 24964813.