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Clinical data | |
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Other names | BIIB-104; PF-04958242 |
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ChemSpider | |
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CompTox Dashboard ( EPA) | |
Chemical and physical data | |
Formula | C18H20N2O4S2 |
Molar mass | 392.49 g·mol−1 |
3D model ( JSmol) | |
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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. [1] [2] [3] 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. [3] [4] As of July 2018, pesampator is in phase II clinical trials for cognitive symptoms in schizophrenia. [3]
Pesampator belongs to the biarylpropylsulfonamide group of AMPAR PAMs, which also includes LY-404187, LY-503430, and mibampator (LY-451395) among others. [5] It is described as a "high-impact" AMPAR PAM, unlike so-called "low-impact" AMPAR PAMs like CX-516 and its congener farampator (CX-691, ORG-24448). [2] In animals, low doses of pesampator have been found to enhance cognition and memory, whereas higher doses produce motor coordination disruptions and convulsions. [2] The same effects, as well as neurotoxicity at higher doses, have been observed with orthosteric and other high-impact allosteric AMPAR activators. [2]
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. [2] It was able to complete reverse ketamine-induced impairments in spatial working memory in the participants. [2]
In addition to its actions on the AMPAR, pesampator has been reported to act as a GlyT1 glycine transporter blocker. [6] [7] 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. [6] [7]
![]() | |
Clinical data | |
---|---|
Other names | BIIB-104; PF-04958242 |
Identifiers | |
| |
CAS Number | |
PubChem CID | |
ChemSpider | |
UNII | |
CompTox Dashboard ( EPA) | |
Chemical and physical data | |
Formula | C18H20N2O4S2 |
Molar mass | 392.49 g·mol−1 |
3D model ( JSmol) | |
| |
|
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. [1] [2] [3] 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. [3] [4] As of July 2018, pesampator is in phase II clinical trials for cognitive symptoms in schizophrenia. [3]
Pesampator belongs to the biarylpropylsulfonamide group of AMPAR PAMs, which also includes LY-404187, LY-503430, and mibampator (LY-451395) among others. [5] It is described as a "high-impact" AMPAR PAM, unlike so-called "low-impact" AMPAR PAMs like CX-516 and its congener farampator (CX-691, ORG-24448). [2] In animals, low doses of pesampator have been found to enhance cognition and memory, whereas higher doses produce motor coordination disruptions and convulsions. [2] The same effects, as well as neurotoxicity at higher doses, have been observed with orthosteric and other high-impact allosteric AMPAR activators. [2]
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. [2] It was able to complete reverse ketamine-induced impairments in spatial working memory in the participants. [2]
In addition to its actions on the AMPAR, pesampator has been reported to act as a GlyT1 glycine transporter blocker. [6] [7] 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. [6] [7]