About: Pesampator

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Pesampator (INN; developmental code names BIIB-104 and PF-04958242) is a positive allosteric modulator (PAM) of the AMPA receptor (AMPAR), an ionotropic glutamate receptor, which is under development by Pfizer for the treatment of cognitive symptoms in schizophrenia. It was also under development for the treatment of age-related sensorineural hearing loss, but development for this indication was terminated due to insufficient effectiveness. As of July 2018, pesampator is in phase II clinical trials for cognitive symptoms in schizophrenia.

Attributes	Values
rdf:type	Thing dul:ChemicalObject chemical substance Drug drug
rdfs:label	Pesampator (en)
rdfs:comment	Pesampator (INN; developmental code names BIIB-104 and PF-04958242) is a positive allosteric modulator (PAM) of the AMPA receptor (AMPAR), an ionotropic glutamate receptor, which is under development by Pfizer for the treatment of cognitive symptoms in schizophrenia. It was also under development for the treatment of age-related sensorineural hearing loss, but development for this indication was terminated due to insufficient effectiveness. As of July 2018, pesampator is in phase II clinical trials for cognitive symptoms in schizophrenia. (en)
foaf:depiction
dct:subject	Experimental drugs Nootropics Nitriles Tetrahydrofurans Thiophenes AMPA receptor positive allosteric modulators Sulfonamides Glycine reuptake inhibitors
Wikipage page ID	55085415 (xsd:integer)
Wikipage revision ID	1082899297 (xsd:integer)
Link from a Wikipage to another Wikipage	Psychotomimetic Schizophrenia Pfizer List of investigational antipsychotics Experimental drugs Memory Co-agonist Glycine Congener (chemistry) Convulsion Clinical trial Positive allosteric modulator Mibampator CX-516 Active site Ageing Ionotropic glutamate receptor Nootropics Extracellular Farampator Glycine receptor Glycine reuptake inhibitor Glycine transporter Motor coordination Nitriles Tetrahydrofurans Thiophenes AMPA receptor AMPA receptor positive allosteric modulator AMPA receptor positive allosteric modulators Sulfonamides Glycine reuptake inhibitors Ketamine LY-404187 LY-503430 Binding site Cognition Working memory Phases of clinical research Regulatory site NMDA receptor Motor disorder Neurotoxicity Sensorineural hearing loss Transporter blocker Biarylpropylsulfonamide GlyT1 Verbal learning Spatial working memory
sameAs	Pesampator Pesampator
dbp:wikiPageUsesTemplate	dbt:Drugbox dbt:Glycine_receptor_modulators dbt:Ionotropic_glutamate_receptor_modulators dbt:Reflist dbt:Abbrlink
thumbnail	wiki-commons:Special:FilePath/BIIB-104.svg?width=300
c	18 (xsd:integer)
CAS number	1258963 (xsd:integer)
ChemSpiderID	32698813 (xsd:integer)
H	20 (xsd:integer)
IUPAC name	N-[-4-[4-phenoxy]oxolan-3-yl]propane-2-sulfonamide (en)
n	2 (xsd:integer)
O	4 (xsd:integer)
PubChem	49853967 (xsd:integer)
s	2 (xsd:integer)
SMILES	CCSN[C@H]1COC[C@H]1OC2=CC=CC3=CC=CC#N (en)
StdInChI	1 (xsd:integer)
StdInChIKey	TTYKUKSFWHEBLI-DLBZAZTESA-N (en)
synonyms	BIIB-104; PF-04958242 (en)
UNII	9 (xsd:integer)
width	250 (xsd:integer)
has abstract	Pesampator (INN; developmental code names BIIB-104 and PF-04958242) is a positive allosteric modulator (PAM) of the AMPA receptor (AMPAR), an ionotropic glutamate receptor, which is under development by Pfizer for the treatment of cognitive symptoms in schizophrenia. It was also under development for the treatment of age-related sensorineural hearing loss, but development for this indication was terminated due to insufficient effectiveness. As of July 2018, pesampator is in phase II clinical trials for cognitive symptoms in schizophrenia. Pesampator belongs to the biarylpropylsulfonamide group of AMPAR PAMs, which also includes LY-404187, LY-503430, and mibampator (LY-451395) among others. It is described as a "high-impact" AMPAR PAM, unlike so-called "low-impact" AMPAR PAMs like CX-516 and its cogener farampator (CX-691, ORG-24448). In animals, low doses of pesampator have been found to enhance cognition and memory, whereas higher doses produce motor coordination disruptions and convulsions. The same effects, as well as neurotoxicity at higher doses, have been observed with orthosteric and other high-impact allosteric AMPAR activators. In healthy volunteers, pesampator has been found to significantly reduce ketamine-induced deficits in verbal learning and working memory without attenuating ketamine-induced psychotomimetic effects. It was able to complete reverse ketamine-induced impairments in spatial working memory in the participants. In addition to its actions on the AMPAR, pesampator has been reported to act as a GlyT1 glycine transporter blocker. As such, it is also a glycine reuptake inhibitor, and may act indirectly to activate the glycine receptor and the glycine co-agonist site of the NMDA receptor by increasing extracellular levels of glycine. (en)
prov:wasDerivedFrom	wikipedia-en:Pesampator?oldid=1082899297&ns=0
page length (characters) of wiki page	7154 (xsd:nonNegativeInteger)
CAS number	1258963-59-5
FDA UNII code	9G1A824CC2
PubChem	49853967
foaf:isPrimaryTopicOf	wikipedia-en:Pesampator
is Link from a Wikipage to another Wikipage of	BIIB-104 C18H20N2O4S2 Sodium- and chloride-dependent glycine transporter 1

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