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In vitro comparison...
In vitro comparison of ulotaront (SEP-363856) and ralmitaront (RO6889450) : two TAAR1 agonist candidate antipsychotics
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- Ågren, Richard (författare)
- Department of Physiology and Pharmacology, Karolinska Institutet, Solna, Sweden
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- Betari, Nibal (författare)
- Umeå universitet,Institutionen för integrativ medicinsk biologi (IMB),Wallenberg centrum för molekylär medicin vid Umeå universitet (WCMM)
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- Saarinen, Marcus (författare)
- Karolinska Institutet
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- Zeberg, Hugo (författare)
- Karolinska Institutet
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- Svenningsson, Per (författare)
- Karolinska Institutet
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- Sahlholm, Kristoffer (författare)
- Karolinska Institutet,Umeå universitet,Institutionen för integrativ medicinsk biologi (IMB),Wallenberg centrum för molekylär medicin vid Umeå universitet (WCMM),Department of Physiology and Pharmacology, Karolinska Institutet, Solna, Sweden
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- Oxford University Press, 2023
- 2023
- Engelska.
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Ingår i: International Journal of Neuropsychopharmacology. - : Oxford University Press. - 1461-1457 .- 1469-5111. ; 26:9, s. 599-606
- Relaterad länk:
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https://doi.org/10.1...
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Ämnesord
Stäng
- BACKGROUND: Trace amine-associated receptor-1 (TAAR1) agonists have been proposed as potential antipsychotics, with ulotaront and ralmitaront having reached clinical trials. While ulotaront demonstrated efficacy in a recent Phase II trial, a corresponding study studies of ralmitaront failed to show efficacy as a monotherapy or as an adjunct to atypical antipsychotics. In addition to TAAR1 agonism, ulotaront is a partial agonist at the serotonin 1A receptor (5-HT1AR). However, little is known about ralmitaront.METHODS: We compared ulotaront and ralmitaront at TAAR1, 5-HT1AR, and dopamine D2 using luciferase complementation-based G protein recruitment, cAMP accumulation, and G protein-coupled inward rectifier potassium channel activation assays.RESULTS: Ralmitaront showed lower efficacy at TAAR1 in G protein recruitment, cAMP accumulation, and GIRK activation assays. Moreover, ralmitaront lacked detectable activity at 5-HT1AR and dopamine D2.CONCLUSIONS: Compared with ulotaront, ralmitaront shows lower efficacy and slower kinetics at TAAR1 and lacks efficacy at 5-HT1AR. These data may be relevant to understanding differences in clinical profiles of these 2 compounds.
Ämnesord
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Farmakologi och toxikologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Pharmacology and Toxicology (hsv//eng)
Nyckelord
- dopamine D2 receptor
- electrophysiology
- luminescence measurements
- serotonin 1A receptor
- Trace amine-associated receptor-1
Publikations- och innehållstyp
- ref (ämneskategori)
- art (ämneskategori)
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