PKR activator 4 (example 7A) 是一种高效的丙酮酸激酶 R (pyruvate kinase R (PKR)) 激活剂，展现出研究血液疾病的潜力。

Metaxalone-D6 is intended for use as an internal standard for the quantification of metaxalone by GC-or LC-MS. Metaxalone (T1610) is a skeletal muscle relaxant. It inhibits the proliferation of,and induces apoptosis in,RAW 264.7 cells in vitro when used at concentrations ranging from 1 to 100 µM. Metaxalone (T1610)also reduces LPS-induced increases in COX-1,COX-2,and NF-kB levels and inhibits LPS-induced production of TNF-α,IL-6,and prostaglandin E2 in RAW 264.7 cells. Formulations containing metaxalone have been used in the treatment of lower back pain.

MK-0952 is a selective PDE4 inhibitor used to treat long-term memory loss and mild cognitive impairment. It is an intrinsically potent inhibitor and has shown limited whole blood activity.

CI-1044 is an inhibitor of PDE4 (IC50s: 0.29, 0.08, 0.56, 0.09 μM for PDE4A5, PDE4B2, PDE4C2 and PDE4D3).

PF-04449613 is a phosphodiesterase 9A (PDE9A) inhibitor (IC50= 22 nM).1It is selective for PDE9A over PDE1C (IC50= >1,000 nM), as well as over a variety of other PDEs, inhibiting PDE2-8, -10, and -11 activity by less than 30% in a panel of enzymes, ion channels, and transporters at 1 μM but does inhibit the human dopamine transporter (DAT; Ki= 293 nM). PF-04449613 (0.1-100 mg/kg, s.c.) increases cerebrospinal fluid (CSF) levels of cyclic GMP (cGMP) in rats. Subcutaneous administration of PF-04449613 (10 mg/kg) increases the rate of dendritic spine formation and elimination in mouse primary motor cortex pyramidal neuronsin vivo.2It increases the average running speed of mice in an accelerating rotarod task, indicating improved motor learning, at the same dose. 1.Claffey, M.M., Helal, C.J., Verhoest, P.R., et al.Application of structure-based drug design and parallel chemistry to identify selective, brain penetrant, in vivo active phosphodiesterase 9A inhibitorsJ. Med. Chem.55(21)9055-90

Kuraridine is measured against cGMP PDE5 to identify potent cGMP specific phosphodiesterase type 5 inhibitory constituents.