Dataset for article: Potent and reversible open-channel blocker of NMDA receptor derived from dizocilpine with enhanced membrane-to-channel inhibition

Figure 1. Synthetic procedure for the preparation of K2060. Reaction conditions: (i) SOCl 2, benzene, 85 ◦C, 2 h; (ii) MeCN, 40 ◦C, 3 h and (iii) HCl (37 % aq.sol.), MeOH, RT, 1 h. 1: 5H -dibenzo[ a,d][7]annulen-5-ol; 2: 5-chloro-5H-dibenzo[a,d][7]annulene; 3: cyclobutanamine, K2060: N-cyclobutyl-5H-dibenzo[a,d][7]annulen-5-amine hydrogen chloride. Figure 2. Values depicted in the accociated article. Results showing K2060 is a potent voltage-dependent inhibitor of GluN1/GluN2 receptors. Figure 3. Values depicted in the accociated article. Results demonstrate that K2060 likely acts as a "partially trapping" open-channel blocker of the GluN1/GluN2A receptor. Fugire 4. Membrane-to-channel inhibition induced by K2060. Figure 5. Results demonstrating that K2060 is a more potent inhibitor of endogenous synaptic NMDARs than memantine. Figure 6. Values demonstrationg the Pharmacokinetics of K2060 and its distribution to the brain. K2060 (10 mg/kg) was administered intraperitoneally to the male mice. Data are visualized as the mean±S.E.M.(n=4). Notethat Tmax(plasma)=5 minutesand Tmax(brain)=15 minutes in the brain, followed by prompt clearance from both compartments. Cmax (plasma)=2947±537 nM;Cmax(brain)=2469±454 nM. Table 1. The IC50 values for inhibitory effects of memantine (Mem )and K2060at the NMDARs. Table 2. The inhibitory kinetics of K2060 at the GluN1/GluN2A receptor. Table 3. Therapeutic efficacy of K2060 (10 mg/kg) in tabun-poisoned mice.