SDZ 220-581

Modify Date: 2024-01-08 18:12:07

SDZ 220-581 Structure
SDZ 220-581 structure
Common Name SDZ 220-581
CAS Number 174575-17-8 Molecular Weight 369.737
Density 1.5±0.1 g/cm3 Boiling Point 613.3±65.0 °C at 760 mmHg
Molecular Formula C16H17ClNO5P Melting Point N/A
MSDS N/A Flash Point 324.7±34.3 °C

 Use of SDZ 220-581


SDZ 220-581 is a potent, competitive antagonist at the NMDA glutamate receptor subtype(pKi= 7.7).IC50 Value: Target: NMDA receptorin 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].

 Names

Name SDZ 220-581,(S)-α-Amino-2'-chloro-5-(phosphonomethyl)[1,1'-biphenyl]-3-propanoicacid
Synonym More Synonyms

 SDZ 220-581 Biological Activity

Description SDZ 220-581 is a potent, competitive antagonist at the NMDA glutamate receptor subtype(pKi= 7.7).IC50 Value: Target: NMDA receptorin 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].
Related Catalog
References

[1]. Gilmour G, Broad LM, Wafford KA, In vitro characterisation of the novel positive allosteric modulators of the mGlu? receptor, LSN2463359 and LSN2814617, and their effects on sleep architecture and operant responding in the rat. Neuropharmacology. 2013 Jan

[2]. Linderholm K, Powell S, Olsson E, Role of the NMDA-receptor in Prepulse Inhibition in the Rat. Int J Tryptophan Res. 2010;3:1-12.

[3]. Urwyler S, Campbell E, Fricker G, Biphenyl-derivatives of 2-amino-7-phosphono-heptanoic acid, a novel class of potent competitive N-methyl-D-aspartate receptor antagonists--II. Pharmacological characterization in vivo. Neuropharmacology. 1996 Jun;35(6):65

[4]. Bakshi VP, Tricklebank M, Neijt HC, Disruption of prepulse inhibition and increases in locomotor activity by competitive N-methyl-D-aspartate receptor antagonists in rats. J Pharmacol Exp Ther. 1999 Feb;288(2):643-52.

 Chemical & Physical Properties

Density 1.5±0.1 g/cm3
Boiling Point 613.3±65.0 °C at 760 mmHg
Molecular Formula C16H17ClNO5P
Molecular Weight 369.737
Flash Point 324.7±34.3 °C
Exact Mass 369.053284
PSA 130.66000
LogP 0.89
Vapour Pressure 0.0±1.9 mmHg at 25°C
Index of Refraction 1.637
Storage condition 2-8℃

 Synonyms

(2S)-2-Amino-3-[2'-chloro-5-(phosphonomethyl)-3-biphenylyl]propanoic acid
sdz 220-581
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