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{{Short description|Chemical compound}} |
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{{drugbox | verifiedrevid = 400102572 |
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{{Drugbox |
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| verifiedrevid = 411533590 |
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| IUPAC_name = (3''R'',5''R'')-5-(3-(cyclopentyloxy)-4-methoxyphenyl)-3-(3-methylbenzyl)piperidin-2-one |
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| IUPAC_name = (3''S'',5''S'')-5-(3-(Cyclopentyloxy)-4-methoxyphenyl)-3-(3-methylbenzyl)piperidin-2-one |
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| image = HT-0712.png |
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| image = HT-0712.svg |
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| width = 160 |
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| width = 250 |
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<!--Clinical data--> |
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| tradename = |
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| pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X --> |
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| pregnancy_US = <!-- A / B / C / D / X --> |
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| pregnancy_category = |
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| legal_AU = <!-- Unscheduled / S2 / S3 / S4 / S5 / S6 / S7 / S8 / S9 --> |
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| legal_CA = <!-- Schedule I --> |
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| legal_UK = <!-- Class A --> |
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| legal_US = <!-- Schedule I --> |
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| legal_status = |
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| routes_of_administration = |
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<!--Pharmacokinetic data--> |
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| bioavailability = |
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| protein_bound = |
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| metabolism = |
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| elimination_half-life = |
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| excretion = |
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<!--Identifiers--> |
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| CAS_number = 617720-02-2 |
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| UNII_Ref = {{fdacite|correct|FDA}} |
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| UNII = 2O43FXG9IG |
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| ATC_prefix = None |
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| ATC_suffix = |
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| PubChem = 9865375 |
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| DrugBank = |
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| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} |
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| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} |
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| ChemSpiderID = 8041067 |
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| ChemSpiderID = 8041067 |
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| InChI = 1/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 |
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<!--Chemical data--> |
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| InChIKey = ABEJDMOBAFLQNJ-NHCUHLMSBI |
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| C=25 | H=31 | N=1 | O=3 |
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| smiles = O=C3NC(c2cc(OC1CCCC1)c(OC)cc2)C3Cc4cccc(c4)C |
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| smiles = O=C3NC(c2cc(OC1CCCC1)c(OC)cc2)C3Cc4cccc(c4)C |
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| StdInChI_Ref = {{stdinchicite|correct|chemspider}} |
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| StdInChI_Ref = {{stdinchicite|correct|chemspider}} |
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| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} |
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| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} |
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| StdInChIKey = ABEJDMOBAFLQNJ-NHCUHLMSSA-N |
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| StdInChIKey = ABEJDMOBAFLQNJ-NHCUHLMSSA-N |
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| synonyms = HT-0712, IPL 455,903 |
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| CAS_number = 617720-02-2 |
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| synonyms = HT-0712, IPL 455,903 |
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| ATC_prefix = |
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| ATC_suffix = |
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| PubChem = 9865375 |
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| DrugBank = |
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| C = 25 | H = 31 | N = 1 | O = 3 |
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| molecular_weight = 393.53 g/mol |
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| bioavailability = |
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| protein_bound = |
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| metabolism = |
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| elimination_half-life = |
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| excretion = |
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| pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X --> |
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| pregnancy_US = <!-- A / B / C / D / X --> |
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| pregnancy_category= |
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| legal_AU = <!-- Unscheduled / S2 / S3 / S4 / S5 / S6 / S7 / S8 / S9 --> |
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| legal_CA = <!-- Schedule I --> |
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| legal_UK = <!-- Class A --> |
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| legal_US = <!-- Schedule I --> |
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| legal_status = |
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| routes_of_administration = |
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}} |
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}} |
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'''HT-0712''' is an experimental ] enhancing ] (]) which is currently undergoing ]. 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. |
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'''HT-0712''', also known as IPL-455903,<ref name="pmid18660832">{{cite journal | vauthors = Giembycz MA | title = Can the anti-inflammatory potential of PDE4 inhibitors be realized: guarded optimism or wishful thinking? | journal = British Journal of Pharmacology | volume = 155 | issue = 3 | pages = 288–290 | date = October 2008 | pmid = 18660832 | pmc = 2567889 | doi = 10.1038/bjp.2008.297 }}</ref> is an experimental ] enhancing ] (]) which is currently undergoing ]. 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.<ref name="pmid17823313">{{cite journal | vauthors = MacDonald E, Van der Lee H, Pocock D, Cole C, Thomas N, VandenBerg PM, Bourtchouladze R, Kleim JA | display-authors = 6 | title = A novel phosphodiesterase type 4 inhibitor, HT-0712, enhances rehabilitation-dependent motor recovery and cortical reorganization after focal cortical ischemia | journal = Neurorehabilitation and Neural Repair | volume = 21 | issue = 6 | pages = 486–496 | year = 2007 | pmid = 17823313 | doi = 10.1177/1545968307305521 | doi-access = free }}</ref> |
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==Mechanism of action== |
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==Mechanism of action== |
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HT-0712 appears to act as a ], thereby increasing ] levels. When cAMP levels are increased in neurons, this may trigger activation of cAMP response element-binding proteins (]). CREBs are ]s involved in the formation of ]. |
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HT-0712 appears to act as a ], thereby increasing ] levels. When cAMP levels are increased in neurons, this may trigger the activation of cAMP response element-binding proteins (]). CREBs are ]s involved in the formation of ].<ref name="pmid17823313"/> |
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The side effects of the drug are not yet fully known. |
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The side effects of the drug are not yet fully known. |
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==Medical use== |
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==Research== |
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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.<ref>{{cite journal | vauthors = Peters M, Bletsch M, Stanley J, Wheeler D, Scott R, Tully T | title = The PDE4 inhibitor HT-0712 improves hippocampus-dependent memory in aged mice | journal = Neuropsychopharmacology | volume = 39 | issue = 13 | pages = 2938–2948 | date = December 2014 | pmid = 24964813 | pmc = 4229572 | doi = 10.1038/npp.2014.154 }}</ref> |
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Middle-aged people, seniors, and possibly those suffering from dementia, who have a hard time remembering everyday events, can possibly benefit from this drug. |
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== References == |
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==Performance enhancing use== |
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{{reflist}} |
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Many students may be inclined to use ] for school and college life for exams and finals. This could also be an effective alternative or adjunctive to the use of ] as a study aid. |
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== External links == |
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==References== |
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==External links== |
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{{pharm-stub}} |
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{{Phosphodiesterase inhibitors}} |
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{{Phosphodiesterase inhibitors}} |
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