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WFRF:(Zhang Hongwen)
 

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LIBRIS Formathandbok  (Information om MARC21)
FältnamnIndikatorerMetadata
00004974naa a2200613 4500
001oai:DiVA.org:lnu-56076
003SwePub
008160831s2016 | |||||||||||000 ||eng|
0247 a https://urn.kb.se/resolve?urn=urn:nbn:se:lnu:diva-560762 URI
0247 a https://doi.org/10.1007/s00213-016-4346-22 DOI
040 a (SwePub)lnu
041 a engb eng
042 9 SwePub
072 7a ref2 swepub-contenttype
072 7a art2 swepub-publicationtype
1001 a Snyder, Gretchen L.u Intra-Cellular Therapies Inc, USA4 aut
2451 0a Preclinical profile of ITI-214, an inhibitor of phosphodiesterase 1, for enhancement of memory performance in rats
264 c 2016-06-24
264 1b Springer Science and Business Media LLC,c 2016
338 a electronic2 rdacarrier
520 a Rationale: Therapeutic agents for memory enhancement in psychiatric disorders, such as schizophrenia, are urgently needed.Objective: The aim of this study is to characterize the preclinical profile of ITI-214, a potent inhibitor of phosphodiesterase 1 (PDE1).Methods: ITI-214 was assayed for inhibition of PDE1 versus other PDE enzyme families using recombinant human PDE enzymes and for off-target binding to 70 substrates (General SEP II diversity panel; Caliper Life Sciences). Effects of ITI-214 (0.1–10 mg/kg, po) on memory performance were assayed in rats using the novel object recognition (NOR) paradigm, with drug given at specified time points prior to or following exposure to objects in an open field. ITI-214 was evaluated for potential drug-drug interaction with risperidone in rats using conditioned avoidance response (CAR) and pharmacokinetic assessments.Results: ITI-214 inhibited PDE1A (Ki = 33 pmol) with >1000-fold selectivity for the nearest other PDE family (PDE4D) and displayed minimal off-target binding interactions in a 70-substrate selectivity profile. By using specific timing of oral ITI-214 administration, it was demonstrated in the NOR that ITI-214 is able to enhance acquisition, consolidation, and retrieval memory processes. All memory effects were in the absence of effects on exploratory behavior. ITI-214 did not disrupt the risperidone pharmacokinetic profile or effects in CAR.Conclusions: ITI-214 improved the memory processes of acquisition, consolidation, and retrieval across a broad dose range (0.1–10 mg/kg, po) without disrupting the antipsychotic-like activity of a clinical antipsychotic medication, specifically risperidone. Clinical development of ITI-214 is currently in progress.
650 7a MEDICIN OCH HÄLSOVETENSKAPx Medicinska och farmaceutiska grundvetenskaperx Farmaceutiska vetenskaper0 (SwePub)301012 hsv//swe
650 7a MEDICAL AND HEALTH SCIENCESx Basic Medicinex Pharmaceutical Sciences0 (SwePub)301012 hsv//eng
650 7a MEDICIN OCH HÄLSOVETENSKAPx Medicinska och farmaceutiska grundvetenskaperx Farmakologi och toxikologi0 (SwePub)301022 hsv//swe
650 7a MEDICAL AND HEALTH SCIENCESx Basic Medicinex Pharmacology and Toxicology0 (SwePub)301022 hsv//eng
653 a Conditioned avoidance response
653 a Cyclic AMP
653 a Cyclic GMP
653 a Memory
653 a Novel object recognition
653 a Phosphodiesterase-1
653 a Pharmacology
653 a Farmakologi
7001 a Prickaerts, Josu Maastricht University, The Netherlands4 aut
7001 a Wadenberg, Marie-Louiseu Linnéuniversitetet,Institutionen för kemi och biomedicin (KOB)4 aut0 (Swepub:lnu)ewamax
7001 a Zhang, Leiu Intra-Cellular Therapies Inc, USA4 aut
7001 a Zheng, Hailinu Intra-Cellular Therapies Inc, USA4 aut
7001 a Yao, Weiu Intra-Cellular Therapies Inc, USA4 aut
7001 a Akkerman, Svenu Maastricht University, The Netherlands4 aut
7001 a Zhu, Hongwenu Tianjin Hospital, China4 aut
7001 a Hendrick, Joseph P.u Intra-Cellular Therapies Inc, USA4 aut
7001 a Vanover, Kimberly E.u Intra-Cellular Therapies Inc, USA4 aut
7001 a Davis, Robertu Intra-Cellular Therapies Inc, USA4 aut
7001 a Li, Pengu Intra-Cellular Therapies Inc, USA4 aut
7001 a Mates, Sharonu Intra-Cellular Therapies Inc, USA4 aut
7001 a Wennogle, Lawrence P.u Intra-Cellular Therapies Inc, USA4 aut
7102 a Intra-Cellular Therapies Inc, USAb Maastricht University, The Netherlands4 org
7730 t Psychopharmacologyd : Springer Science and Business Media LLCg 233:17, s. 3113-3124q 233:17<3113-3124x 0033-3158x 1432-2072
8564 u https://doi.org/10.1007/s00213-016-4346-2y Fulltext
8564 u http://rdcu.be/o9GCy Fulltext (read only)
8564 u https://lnu.diva-portal.org/smash/get/diva2:971432/FULLTEXT01.pdfx primaryx Raw objecty fulltext:print
8564 u https://link.springer.com/content/pdf/10.1007%2Fs00213-016-4346-2.pdf
8564 8u https://urn.kb.se/resolve?urn=urn:nbn:se:lnu:diva-56076
8564 8u https://doi.org/10.1007/s00213-016-4346-2

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