Product Details of 136725-55-8. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: (R)-(-)-3-Fluoropyrrolidine Hydrochloride, is researched, Molecular C4H9ClFN, CAS is 136725-55-8, about Discovery of a pyrazolo[1,5-a]pyrimidine derivative (MT-3014) as a highly selective PDE10A inhibitor via core structure transformation from the stilbene moiety. Author is Koizumi, Yuuki; Tanaka, Yoshihito; Matsumura, Takehiko; Kadoh, Yoichi; Miyoshi, Haruko; Hongu, Mitsuya; Takedomi, Kei; Kotera, Jun; Sasaki, Takashi; Taniguchi, Hiroyuki; Watanabe, Yumi; Takakuwa, Misae; Kojima, Koki; Baba, Nobuyuki; Nakamura, Itsuko; Kawanishi, Eiji.
We have developed a new class of PDE10A inhibitor, a pyrazolo[1,5-a]pyrimidine derivative MT-3014 (1, I). A previous compound introduced was deprioritized due to concerns for E/Z-isomerization and glutathione-adduct formation at the core stilbene structure. We discovered pyrazolo [1,5-a] pyrimidine as a new lead scaffold by structure-based drug design utilizing a co-crystal structure with PDE10A. The lead compound was optimized for in vitro activity, solubility, and selectivity against human ether-a-́go-go related gene cardiac channel binding. We observed that I shows excellent efficacy in rat conditioned avoidance response test and suitable pharmacokinetic properties in rats, especially high brain penetration.
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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem