Uses
DL-AP5 (2-APV) lithium is a competitive NMDA (N-methyl-D-aspartate) receptor antagonist. DL-AP5 lithium shows significantly antinociceptive activity. DL-AP5 lithium specifically blocks on channels in the rabbit retina[1][2][3].
Biological Activity
DL-2-Amino-5-phosphonovaleric acid is a selective N-methyl-d-aspartate (NMDA) receptor antagonist used frequently in studies of neurological processes', 'Anticonvulsant; potent and selective antagonist for NMDA receptors.
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 (10-2 μg/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. |
References
[1] Murray CW, et al. Neurokinin and NMDA antagonists (but not a kainic acid antagonist) are antinociceptive in the mouse formalin model. Pain. 1991;44(2):179-185. DOI:10.1016/0304-3959(91)90135-K
[2] Massey SC, et al. N-methyl-D-aspartate receptors of ganglion cells in rabbit retina. J Neurophysiol. 1990;63(1):16-30. DOI:10.1152/jn.1990.63.1.16
[3] Jafari-Sabet M. NMDA receptor blockers prevents the facilitatory effects of post-training intra-dorsal hippocampal NMDA and physostigmine on memory retention of passive avoidance learning in rats. Behav Brain Res. 2006 Apr 25;169(1):120-7. DOI:10.1016/j.bbr.2005.12.011
[4] Taati M, et al. The effects of DL-AP5 and glutamate on ghrelin-induced feeding behavior in 3-h food-deprived broiler cockerels. J Physiol Biochem. 2011 Jun;67(2):217-23. DOI:10.1007/s13105-010-0066-y
[5] Chen T, et al. Glutamate-induced rapid induction of Arc/Arg3.1 requires NMDA receptor-mediated phosphorylation of ERK and CREB. Neurosci Lett. 2017 Nov 20;661:23-28. DOI:10.1016/j.neulet.2017.09.024
