Ro 25-6981 maleate
Modify Date: 2024-01-03 10:57:02
Ro 25-6981 maleate structure
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Common Name | Ro 25-6981 maleate | ||
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| CAS Number | 1312991-76-6 | Molecular Weight | 455.543 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C26H33NO6 | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | N/A | |
| Symbol |
GHS07, GHS09 |
Signal Word | Warning | |
Use of Ro 25-6981 maleateRo 25-6981 Maleate is a potent and selective activity-dependent blocker of NMDA receptors containing the NR2B subunit. IC50 values are 0.009 and 52 μM for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A respectively.IC50 value: 9 nM [1]Target: NMDA receptor subtype of NR1C & NR2Bin vitro: Ro 25-6981 inhibited 3H-MK-801 binding to rat forebrain membranes in a biphasic manner with IC50 values of 0.003 microM and 149 microM for high- (about 60%) and low-affinity sites, respectively. NMDA receptor subtypes expressed in Xenopus oocytes were blocked with IC50 values of 0.009 microM and 52 microM for the subunit combinations NR1C & NR2B and NR1C & NR2A, respectively, which indicated a >5000-fold selectivity [1]. Increasing the concentration of spermidine did not change the efficacy of RO 25-6981 and minimally changed the IC(50) value. Epsilon1Q336R receptors were more inhibited by ifenprodil and RO 25-9681 than wildtype epsilon1 receptors in ligand binding assays but not in functional assays [2].in vivo: Intrathecal injection of Ro 25-6981 significantly enhanced the paw withdrawal mechanical threshold and paw withdrawal thermal latency after the operation. Significant change has been observed after intrathecal injection of 800.0 μg of Ro 25-6981 and at 2h after operation in the oblique pull test degree and BBB rating score. Pretreatment of Ro 25-6981 decreased the high level expression of NR2B with tyrosine phosphorylation in spinal dorsal horn of the rat model after the operation [3]. |
| Name | Ro 25-6981 Maleate |
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| Synonym | More Synonyms |
| Description | Ro 25-6981 Maleate is a potent and selective activity-dependent blocker of NMDA receptors containing the NR2B subunit. IC50 values are 0.009 and 52 μM for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A respectively.IC50 value: 9 nM [1]Target: NMDA receptor subtype of NR1C & NR2Bin vitro: Ro 25-6981 inhibited 3H-MK-801 binding to rat forebrain membranes in a biphasic manner with IC50 values of 0.003 microM and 149 microM for high- (about 60%) and low-affinity sites, respectively. NMDA receptor subtypes expressed in Xenopus oocytes were blocked with IC50 values of 0.009 microM and 52 microM for the subunit combinations NR1C & NR2B and NR1C & NR2A, respectively, which indicated a >5000-fold selectivity [1]. Increasing the concentration of spermidine did not change the efficacy of RO 25-6981 and minimally changed the IC(50) value. Epsilon1Q336R receptors were more inhibited by ifenprodil and RO 25-9681 than wildtype epsilon1 receptors in ligand binding assays but not in functional assays [2].in vivo: Intrathecal injection of Ro 25-6981 significantly enhanced the paw withdrawal mechanical threshold and paw withdrawal thermal latency after the operation. Significant change has been observed after intrathecal injection of 800.0 μg of Ro 25-6981 and at 2h after operation in the oblique pull test degree and BBB rating score. Pretreatment of Ro 25-6981 decreased the high level expression of NR2B with tyrosine phosphorylation in spinal dorsal horn of the rat model after the operation [3]. |
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| Related Catalog | |
| References |
| Molecular Formula | C26H33NO6 |
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| Molecular Weight | 455.543 |
| Exact Mass | 455.230774 |
| PSA | 118.30000 |
| LogP | 3.66610 |
| Storage condition | 2-8℃ |
| Symbol |
GHS07, GHS09 |
|---|---|
| Signal Word | Warning |
| Hazard Statements | H315-H319-H335-H400 |
| Precautionary Statements | P261-P273-P305 + P351 + P338 |
| RIDADR | UN 3077 9 / PGIII |
| 1-Piperidinepropanol, α-(4-hydroxyphenyl)-β-methyl-4-(phenylmethyl)-, (αR,βS)-, (2Z)-2-butenedioate (1:1) (salt) |
| 4-[(1R,2S)-3-(4-Benzylpiperidin-1-yl)-1-hydroxy-2-methylpropyl]phenol (2Z)-but-2-enedioate (1:1) |
| 4-[(1R,2S)-3-(4-Benzyl-1-piperidinyl)-1-hydroxy-2-methylpropyl]phenol (2Z)-2-butenedioate (1:1) |
| 1-Piperidinepropanol |
| Ro 25-6981 (Maleate) |