DL-AP5 (2-APV) 是一种竞争性的NMDA(N-methyl-D-aspartate) 受体拮抗剂。DL-AP5 表现出明显的镇痛活性。DL-AP5 可特异性阻断兔视网膜的通道。
生物活性 | DL-AP5 (2-APV) is a competitiveNMDA(N-methyl-D-aspartate) receptor antagonist. DL-AP5 shows significantly antinociceptive activity. DL-AP5 specifically blocks on channels in the rabbit retina[1][2][3]. |
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体外研究 (In Vitro) | DL-AP5 (100 μM) partially prevents glutamate-induced increase in Arc/Arg3.1 protein levels[5]. DL-AP5 decreases the NMDA-induced Arc/Arg3.1 upregulation[5].
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体内研究 (In Vivo) | DL-AP5 (0-10 μg/rat, Intra-CA1) significantly decreases the effect of NMDA[3]. DL-AP5 (0-10 nmol, Intracerebroventricular injection) causes a dose-dependent increase in food consumption[4]. DL-AP5 (5 nmol, Intracerebroventricular injection) attenuates the decreased food consumption induced by the intracerebroventricular injection of ghrelin[4].
Animal Model: | Male Wistar rats (180-230 g)[3] | Dosage: | 1, 3.2 and 10 μg/rat | Administration: | Injected into the intra-dorsal hippocampal (intra-CA1) immediately after shock administration, once | Result: | Significantly decreased the effect of NMDA (10-2μg/rat, intra-CA1) with significant interaction. |
Animal Model: | Broilers cockerels (3-h fooddeprived (FD3), n=8 for each group)[4] | Dosage: | 0, 2.5, 5, and 10 nmol; in a volume of 10 μL | Administration: | Intracerebroventricular injection | Result: | Caused a dose-dependent increase in food consumption which was significant for 5 and 10 nmol doses. |
Animal Model: | Broilers cockerels (3-h fooddeprived (FD3), n=8 for each group)[4] | Dosage: | 5 nmol | Administration: | Intracerebroventricular injection, followed by ghrelin (0.6 nmol) | Result: | Attenuated the decreased food consumption induced by the intracerebroventricular injection of ghrelin. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: H2O : 33.33 mg/mL(169.08 mM;ultrasonic and warming and heat to 60℃) 配制储备液 1 mM | 5.0728 mL | 25.3640 mL | 50.7279 mL | 5 mM | 1.0146 mL | 5.0728 mL | 10.1456 mL | 10 mM | 0.5073 mL | 2.5364 mL | 5.0728 mL |
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