E-viri
Recenzirano
-
Hao, Junliang; Beck, James; Zhou, Xin; Lackner, Gregory L; Johnston, Richard; Reinhard, Matt; Goldsmith, Paul; Hollinshead, Sean; Dehlinger, Veronique; Filla, Sandra A; Wang, Xu-Shan; Richardson, Jeffery; Posada, Maria; Mohutsky, Mike; Schober, Doug; Katner, Jason S; Chen, Qi; Hu, Bingjie; Remick, David M; Coates, David A; Mathes, Brian M; Hawk, Mai K; Svensson, Kjell A; Hembre, Erik
Journal of medicinal chemistry, 03/2022, Letnik: 65, Številka: 5Journal Article
Results from recently completed clinical studies suggest the dopamine D1 receptor positive allosteric modulator (PAM) mevidalen ( ) could offer unique value for lewy body dementia (LBD) patients. In nonclinical assessments, was mainly eliminated by CYP3A4-mediated metabolism, therefore at the risk of being a victim of drug-drug interactions (DDI) with CYP3A4 inhibitors and inducers. An effort was initiated to identify a new D1 PAM with an improved DDI risk profile. While attempts to introduce additional metabolic pathways mediated by other CYP isoforms failed to provide molecules with an acceptable profile, we discovered that the relative contribution of CYP-mediated oxidation and UGT-mediated conjugation could be tuned to reduce the CYP3A4-mediated victim DDI risk. We have identified LY3154885 ( ), a D1 PAM that possesses similar in vitro and in vivo pharmacologic properties as , but is metabolized mainly by UGT, predicting it could potentially offer lower victim DDI risk in clinic.
Avtor
![loading ... loading ...](themes/default/img/ajax-loading.gif)
Vnos na polico
Trajna povezava
- URL:
Faktor vpliva
Dostop do baze podatkov JCR je dovoljen samo uporabnikom iz Slovenije. Vaš trenutni IP-naslov ni na seznamu dovoljenih za dostop, zato je potrebna avtentikacija z ustreznim računom AAI.
Leto | Faktor vpliva | Izdaja | Kategorija | Razvrstitev | ||||
---|---|---|---|---|---|---|---|---|
JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
Baze podatkov, v katerih je revija indeksirana
Ime baze podatkov | Področje | Leto |
---|
Povezave do osebnih bibliografij avtorjev | Povezave do podatkov o raziskovalcih v sistemu SICRIS |
---|
Vir: Osebne bibliografije
in: SICRIS
To gradivo vam je dostopno v celotnem besedilu. Če kljub temu želite naročiti gradivo, kliknite gumb Nadaljuj.