HT-0712

HT-0712
Identifiers

IUPAC name (3S,5S)-5-(3-(Cyclopentyloxy)-4-methoxyphenyl)-3-(3-methylbenzyl)piperidin-2-one
Synonyms	HT-0712, IPL 455,903
CAS Number	617720-02-2
PubChem (CID)	9865375
ChemSpider	8041067^Y
Chemical and physical data
Formula	C₂₅H₃₁NO₃
Molar mass	393.53 g/mol
3D model (Jmol)	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
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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 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?". Br. J. Pharmacol. 155 (3): 288–90. doi:10.1038/bjp.2008.297. PMC 2567889. PMID 18660832.
1 2 MacDonald E, Van der Lee H, Pocock D, et al. (2007). "A novel phosphodiesterase type 4 inhibitor, HT-0712, enhances rehabilitation-dependent motor recovery and cortical reorganization after focal cortical ischemia". Neurorehabil Neural Repair. 21 (6): 486–96. doi:10.1177/1545968307305521. PMID 17823313.
↑ "The PDE4 inhibitor HT-0712 improves hippocampus-dependent memory in aged mice". Retrieved 18 October 2015.

External links

PDE inhibitors

PDE1	MMPX SCH-51866 Vinpocetine

PDE2	BAY 60-7550 EHNA Oxindole PDP

PDE3	Adibendan Amrinone (inamrinone) Anagrelide Bucladesine Cilostamide Cilostazol Enoximone Imazodan KMUP-1 Meribendan Milrinone Olprinone Parogrelil Pimobendan Quazinone RPL-554 Siguazodan Tetomilast Tofimilast Trequinsin Vesnarinone

PDE4	Apremilast Arofylline Atizoram Catramilast CC-1088 CDP-840 CGH-2466 Cilomilast Cipamfylline CP-80633 Crisaborole Denbutylline Drotaverine Etazolate Filaminast Glaucine HT-0712 ICI-63197 Indimilast Irsogladine Lavamilast Lirimilast Luteolin Mesembrenone Mesembrine Mesopram Oglemilast Piclamilast Revamilast Ro 20-1724 Roflumilast Rolipram Ronomilast RPL-554 RS-25344 YM-976

PDE5	Acetildenafil Aildenafil Avanafil Beminafil Benzamidenafil Dasantafil Icariin Gisadenafil Homosildenafil Lodenafil Mirodenafil MY-5445 Nitrosoprodenafil Sildenafil Sulfoaildenafil T-0156 Tadalafil Udenafil Vardenafil

PDE7	BRL-50481

PDE9	BAY 73-6691 PF-04447943

PDE10	Papaverine PF-2545920 TC-E 5005 Tofisopam

PDE11	BC11-38

Non-selective	Aminophylline Caffeine Choline theophyllinate CPX Dipyridamole Doxofylline Enprofylline Ibudilast IBMX Luteolin Paraxanthine Pentoxifylline Propentofylline SCH-51866 Theobromine Theophylline Zaprinast Zardaverine

Unsorted	Benafentrine Carbazeran Diazepam Diphylline Doxofylline DPCPX Furafylline Lisofylline MDL-12330A Moxaverine Oxagrelate Pentifylline Proxyphylline Pumafentrine Quercetin Satigrel Tolafentrine Trapidil

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