| 词条 | Unifiram |
| 释义 |
| Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 376279547 | IUPAC_name = 2-[(4-Fluorophenyl)sulfonyl]hexahydropyrrolo[1,2-a]pyrazin-6(2H)-one | image = Unifiram.svg | alt = Skeletal formula | image2 = Unifiram molecule ball.png | alt2 = Ball-and-stick model of unifiram | width = 240 | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = Unscheduled | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | excretion = | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 272786-64-8 | ATC_prefix = | ATC_suffix = | PubChem = 9861054 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = | ChEMBL_Ref = {{ebicite|changed|EBI}} | ChEMBL = 140717 | ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}} | ChemSpiderID = 8036753 | UNII = N4024LN29G | UNII_Ref = {{fdacite|changed|FDA}} | synonyms = DM-232 | C=13 | H=15 | F=1 | N=2 | O=3 | S=1 | molecular_weight = 298.333 g/mol | SMILES = C2CN1C(=O)CCC1CN2S(=O)(=O)c(cc3)ccc3F | StdInChI_Ref = {{stdinchicite|changed|chemspider}} | StdInChI = 1S/C13H15FN2O3S/c14-10-1-4-12(5-2-10)20(18,19)15-7-8-16-11(9-15)3-6-13(16)17/h1-2,4-5,11H,3,6-9H2 | StdInChIKey_Ref = {{stdinchicite|changed|chemspider}} | StdInChIKey = SNRTZFZAFBIBJP-UHFFFAOYSA-N }}Unifiram (developmental code name DM-232) is an experimental drug.[1] that has antiamnesic and other effects in animal studies with far greater potency than piracetam.[2][3] A number of related compounds are known, such as sunifiram (DM-235) and sapunifiram (MN-19).[4][5][6] Unifiram has two enantiomers, with the dextro form being the more active isomer.[7] It has been shown to reduce the duration of hypnosis induced by pentobarbital, without impairing motor coordination.[8] {{As of|2015}}, no formal human studies with unifiram have been conducted. Unifiram is not patented and, despite the lack of human and long-term toxicity studies, it is commonly sold online.[9] PharmacologyUnifiram, as well as sunifiram, were assayed at a wide panel of sites, including the most important receptors, ion channels, and transporters, but showed no affinity for any of the sites.[9][10] They specifically did not bind to the glutamate, GABA, serotonin, dopamine, adrenergic, histamine, acetylcholine, or opioid receptors at concentrations of up to 1 μM.[9][10] In addition, the drugs were tested on recombinant AMPA receptors and showed no potentiation of the receptors, indicating that they do not act as AMPA receptor positive allosteric modulators.[9] However, they were able to prevent the amnesia induced by the AMPA receptor antagonist NBQX in the passive avoidance test, suggesting that indirect/downstream AMPA receptor activation may be involved in their memory-enhancing effects.[10] ChemistryReferences1. ^{{Cite journal| last1 = Galeotti | first1 = N.| last2 = Ghelardini | first2 = C.| last3 = Pittaluga | first3 = A.| last4 = Pugliese | first4 = A.| last5 = Bartolini | first5 = A.| last6 = Manetti | first6 = D.| last7 = Romanelli | first7 = M.| last8 = Gualtieri | first8 = F.| title = AMPA-receptor activation is involved in the antiamnesic effect of DM 232 (unifiram) and DM 235 (sunifiram)| journal = Naunyn-Schmiedeberg's Archives of Pharmacology| volume = 368| issue = 6| pages = 538–545| year = 2003| pmid = 14600801| doi = 10.1007/s00210-003-0812-6}} {{Nootropics}}2. ^{{Cite journal| last1 = Ghelardini | first1 = C.| last2 = Galeotti | first2 = N.| last3 = Gualtieri | first3 = F.| last4 = Romanelli | first4 = M.| last5 = Bucherelli | first5 = C.| last6 = Baldi | first6 = E.| last7 = Bartolini | first7 = A.| title = DM235 (sunifiram): a novel nootropic with potential as a cognitive enhancer| journal = Naunyn-Schmiedeberg's Archives of Pharmacology| volume = 365| issue = 6| pages = 419–426| year = 2002| pmid = 12070754| doi = 10.1007/s00210-002-0577-3| hdl = 2158/772195}} 3. ^{{Cite journal| last1 = Romanelli | first1 = M.| last2 = Galeotti | first2 = N.| last3 = Ghelardini | first3 = C.| last4 = Manetti | first4 = D.| last5 = Martini | first5 = E.| last6 = Gualtieri | first6 = F.| title = Pharmacological characterization of DM232 (unifiram) and DM235 (sunifiram), new potent cognition enhancers| journal = CNS Drug Reviews| volume = 12| issue = 1| pages = 39–52| year = 2006| pmid = 16834757| doi = 10.1111/j.1527-3458.2006.00039.x}} 4. ^{{Cite journal| pmid = 14697772| year = 2004| last1 = Scapecchi | first1 = S.| last2 = Martini| last3 = Manetti| last4 = Ghelardini| last5 = Martelli| last6 = Dei| last7 = Galeotti| last8 = Guandalini| last9 = Novella Romanelli| title = Structure-activity relationship studies on unifiram (DM232) and sunifiram (DM235), two novel and potent cognition enhancing drugs| volume = 12| issue = 1| pages = 71–85 | first10 = E.| journal = Bioorganic & Medicinal Chemistry| doi = 10.1016/j.bmc.2003.10.025 | first2 = E.| last10 = Teodori | first3 = D. | first4 = C. | first5 = C. | first6 = S. | first7 = N. | first8 = L. | first9 = M.}} 5. ^{{Cite journal| last1 = Martini | first1 = E.| last2 = Ghelardini | first2 = C.| last3 = Dei | first3 = S.| last4 = Guandalini | first4 = L.| last5 = Manetti | first5 = D.| last6 = Melchiorre | first6 = M.| last7 = Norcini | first7 = M.| last8 = Scapecchi | first8 = S.| last9 = Teodori | first9 = E.| last10 = Romanelli | first10 = M. N.| title = Design, synthesis and preliminary pharmacological evaluation of new piperidine and piperazine derivatives as cognition-enhancers| journal = Bioorganic & Medicinal Chemistry| volume = 16| issue = 3| pages = 1431–1443| year = 2008| pmid = 17981042| doi = 10.1016/j.bmc.2007.10.050}} 6. ^{{Cite journal| last3 = Ghelardini| last4 = Manetti | first1 = E.| last2 = Norcini| first2 = M.| last9 = Scapecchi | first3 = C.| last6 = Guandalini | first4 = D.| first5 = S.| last8 = Pagella| last5 = Dei| last1 = Martini | first6 = L.| first7 = M.| first8 = S.| last7 = Melchiorre| first9 = S.| title = Design, synthesis and preliminary pharmacological evaluation of new analogues of DM232 (unifiram) and DM235 (sunifiram) as cognition modulators| journal = Bioorganic & Medicinal Chemistry| volume = 16| issue = 23| pages = 10034–10042| year = 2008| doi = 10.1016/j.bmc.2008.10.017| pmid = 18954993 | first10 = E.|last10=Teodoria}} 7. ^{{Cite journal | doi = 10.2174/1573406054864142 | pmid = 16787332 | year = 2005 | last1 = Martini | first1 = E. | last2 = Ghelardini | first2=C.| last3 = Bertucci | first3=C.| last4 = Dei | first4=S.| last5 = Gualtieri | first5=F.| last6 = Guandalini | first6=L.| last7 = Manetti | first7=D.| last8 = Scapecchi | first8=S.| last9 = Teodori | first9=E.| title = Enantioselective synthesis and preliminary pharmacological evaluation of the enantiomers of unifiram (DM232), a potent cognition-enhancing agent | volume = 1 | issue = 5 | pages = 473–480 | journal = Medicinal Chemistry| first10 = M. N.| last10 = Romanelli}} 8. ^{{Cite journal | last1 = Ghelardini | first1 = C. | last2 = Galeotti | first2 = N. | last3 = Gualtieri | first3 = F. | last4 = Manetti | first4 = D. | last5 = Bucherelli | first5 = C. | last6 = Baldi | first6 = E. | last7 = Bartolini | first7 = A. | title = The novel nootropic compound DM232 (UNIFIRAM) ameliorates memory impairment in mice and rats | doi = 10.1002/ddr.10055 | journal = Drug Development Research | volume = 56 | pages = 23–32 | year = 2002 | pmid = | pmc = | hdl = 2158/772162 }} 9. ^1 2 3 {{cite journal | vauthors = Gualtieri F | title = Unifi nootropics from the lab to the web: a story of academic (and industrial) shortcomings | journal = J Enzyme Inhib Med Chem | volume = 31 | issue = 2 | pages = 187–94 | year = 2016 | pmid = 25831025 | doi = 10.3109/14756366.2015.1021252 | url = }} 10. ^1 2 {{cite journal | vauthors = Romanelli MN, Galeotti N, Ghelardini C, Manetti D, Martini E, Gualtieri F | title = Pharmacological characterization of DM232 (unifiram) and DM235 (sunifiram), new potent cognition enhancers | journal = CNS Drug Rev | volume = 12 | issue = 1 | pages = 39–52 | year = 2006 | pmid = 16834757 | doi = 10.1111/j.1527-3458.2006.00039.x | url = }} 5 : Designer drugs|Drugs with unknown mechanisms of action|Fluoroarenes|Nootropics|Pyrrolopyrazines |
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