SDZ 220-581 是一种具有口服活性、强效、竞争性 NMDA 受体拮抗剂,pKi 值为 7.7。
Cas No. | 174575-17-8 |
别名 | (S)-ALPHA-氨基-2'-氯-5-(膦酰基甲基)-[1,1'-联苯]-3-丙酸,SDZ 220 581 |
化学名 | 2-amino-3-(2'-chloro-5-(phosphonomethyl)-[1,1'-biphenyl]-3-yl)propanoic acid |
Canonical SMILES | O=P(O)(O)CC1=CC(C2=CC=CC=C2Cl)=CC(CC(N)C(O)=O)=C1 |
分子式 | C16H17ClNO5P |
分子量 | 369.74 |
溶解度 | Soluble in DMSO |
储存条件 | Store at -20℃ |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | Description:
IC50 Value: N/A
SDZ 220-581 ((S)-alpha-amino 2'chloro-5-(phosphonomethyl)[1,1'-biphenyl]-3-propanoic acid) is a potent, competitive antagonist at the NMDA glutamate receptor subtype.
in vitro: Wake-promoting doses of LSN2463359 and LSN2814617 attenuated deficits in performance induced by the competitiveNMDA receptor antagonist SDZ 220,581 in two tests of operant behaviour: the variable interval 30 s task and the DMTP task [1].
in vivo: Administration of SDZ 220-581 or CGS 19755 was associated with a robust reduction in PPI, whereas L-701,324, 4-Cl-KYN or MLA failed to alter PPI [2]. With the most active agent, SDZ 220-581, full protection against maximal electroshock seizures (MES) was obtained at oral doses of 10 mg/kg in rats and in mice. The compound had a fast onset (< or = 1 hr) and a long duration (> or = 24 hr) of action [3]. Rats were pretreated with clozapine (0 or 5.0 mg/kg) or haloperidol (0 or 0.1 mg/kg), together with SDZ 220-581 (0 or 2.5 mg/kg), and tested. SDZ 220-581 and SDZ EAB-515 decreased PPI without affecting startle magnitude [4].
Clinical trial: N/A |