SDZ 220-581

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

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].

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

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	Signaling Pathways >> Membrane Transporter/Ion Channel >> iGluR Signaling Pathways >> Neuronal Signaling >> iGluR Research Areas >> Neurological Disease
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.

Description

Related Catalog

Signaling Pathways >> Membrane Transporter/Ion Channel >> iGluR

Signaling Pathways >> Neuronal Signaling >> iGluR

Research Areas >> Neurological Disease

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.

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℃

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

sdz 220-581

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China
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China
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Purity: 98.0%
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SDZ 220-581

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