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| '''AP-7''' is a selective ] that ] the glutamate binding site and thus activation of ]. It has ] effects.<ref>Meldrum B, Millan M, Patel S, de Sarro G. Anti-epileptic effects of focal micro-injection of excitatory amino acid antagonists. ''Journal of Neural Transmission''. 1988;72(3):191-200. PMID 3047315</ref> | '''AP-7''' is a selective ] that ] the glutamate binding site and thus activation of ]. It has ] effects.<ref>Meldrum B, Millan M, Patel S, de Sarro G. Anti-epileptic effects of focal micro-injection of excitatory amino acid antagonists. ''Journal of Neural Transmission''. 1988;72(3):191-200. PMID 3047315</ref> | ||
| Studies found that '''AP-7''' injected directly into the dorsal periaqueductal grey (DPAG) of rats produced an anxiolytic effect, whereas direct injection outside of the DPAG did not elicit anxiolytic effects. This suggests that a portion of systemically taken NMDA antagonist’s anxiolytic effects comes from the DPAG region of the brain, at least in rats.<sup>2</sup> | |||
| The DPAG are of the brain is thought to deal with fear-like defensive behavior via NMDA and glycine B receptors.<sup>3</sup> These excitatory glutamate receptors work with the inhibitory GABA receptors to achieve equilibrium in the brain.<sup>4</sup> | |||
| '''AP-7''' has been known to cause muscle rigidity and catalepsy in rats following bilateral microinjections (0.02-0.5 nmol) into the globus pallidus and ventral-posterior portions of the caudate-putamen.<sup>5</sup> | |||
| A form of '''AP-7''', D-(-)-2-amino-7-phosphonoheptanoic acid , has also been researched. In groups of hypoxia-treated rats, D-AP7 enhanced motility, exhibited anxiogenic-like effect and impaired consolidation in passive avoidance. Both '''AP-7''' and D-AP7 function as potent, specific antagonists of the NMDA receptor.<sup>6</sup> | |||
| '''AP-7''' functions specifically as a NMDA recognition site blocker, in contrast with 7c-KYNA which acts as a glycine site modulation blocker.<sup>7</sup> | |||
| '''ABBREVIATIONS''' | |||
| '''AP-7''' 2-amino-7-phosphonoheptanoate (a NMDA recognition site blocker) | |||
| '''7-cKYNA''', 7-chlorokynurenate (an NMDA glycine site antagonist) | |||
| ==See also== | ==See also== | ||
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| ==References== | ==References== | ||
| <references/> | <references/> | ||
| 2. “Anxiolytic effect in the elevated plus-maze of the NMDA receptor antagonist AP7 microinjected into the dorsal periaqueductal grey.” Guimarães FS, Carobrez AP, De Aguiar JC, Graeff FG. Department of Pharmacology, FMRP, University of São Paulo, Ribeirão Preto, Brazil. Psychopharmacology (Berl). 1991;103(1):91-4. PMID: 1672463 http://www.ncbi.nlm.nih.gov/pubmed/1672463 | |||
| 3. “Modulation of defensive behavior by periaqueductal gray NMDA/glycine-B receptor.” Carobrez AP, Teixeira KV, Graeff FG. Departamento de Farmacologia/CCB, Universidade Federal de Santa Catarina, SC 88040-900, Florianópolis, Brazil. adepadua@farmaco.ufsc.br Neurosci Biobehav Rev. 2001 Dec;25(7-8):697-709. PMID: 11801295 http://www.ncbi.nlm.nih.gov/pubmed/11801295 | |||
| 4. “The effect of baclofen and AP-7 on selected behavior in rats.” Car H, Wiśniewski K. Department of Pharmacology, Medical Academy in Białystok, Poland. Pharmacol Biochem Behav. 1998 Mar;59(3):685-9. PMID: 9512072 http://www.ncbi.nlm.nih.gov/pubmed/9512072 | |||
| 5. “Blockade of excitatory neurotransmission in the globus pallidus induces rigidity and akinesia in the rat: implications for excitatory neurotransmission in pathogenesis of Parkinson's diseases.” Turski L, Klockgether T, Turski WA, Schwarz M, Sontag KH Max-Planck Institute for Experimental Medicine, Göttingen, F.R.G. Brain Research Type: Journal Article, Research Support, Non-U.S. Gov't DOI: 10.1016/0006-8993(90)91180-O http://ukpmc.ac.uk/abstract/MED/2159826/reload=0;jsessionid=XgXmGdR8IOBFiuG26uSS.2 http://www.sciencedirect.com/science/article/pii/000689939091180O | |||
| 6. “Behavioral effects of D-AP7 in rats subjected to experimental hypoxia.” Nadlewska A, Car H, Wiśniewska R, Hoły Z, Wiśniewski K. Department of Pharmacology, Medical Academy, Mickiewicza 2c, PL 15-222 Białystok, Poland. Pol J Pharmacol. 2003 May-Jun;55(3):337-44. PMID: 14506312 http://www.ncbi.nlm.nih.gov/pubmed/14506312 | |||
| 7. “Quinolinic acid, the inescapable neurotoxin.” Guillemin GJ. Department of Pharmacology, School of Medical Sciences, University of New South Wales, Sydney, NSW, Australia. g.guillemin@unsw.edu.au FEBS J. 2012 Apr;279(8):1356-65. doi: 10.1111/j.1742-4658.2012.08485.x. Epub 2012 Mar 27. | |||
| {{Glutamate_receptor_ligands}} | {{Glutamate_receptor_ligands}} | ||
Revision as of 16:34, 19 October 2012
For other uses, see AP-7 (disambiguation).
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| Names | |
|---|---|
| IUPAC name 2-amino-7-phosphonoheptanoic acid | |
| Identifiers | |
| CAS Number | |
| 3D model (JSmol) | |
| ChEMBL | |
| ChemSpider | |
| PubChem CID | |
| CompTox Dashboard (EPA) | |
InChI
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SMILES
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| Properties | |
| Chemical formula | C7H16NO5P |
| Molar mass | 225.179 g/mol |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C , 100 kPa).
 Y verify (what is ?)
Infobox references
| |
AP-7 is a selective NMDA receptor (NMDAR) antagonist that competitively inhibits the glutamate binding site and thus activation of NMDAR. It has anticonvulsant effects.
Studies found that AP-7 injected directly into the dorsal periaqueductal grey (DPAG) of rats produced an anxiolytic effect, whereas direct injection outside of the DPAG did not elicit anxiolytic effects. This suggests that a portion of systemically taken NMDA antagonist’s anxiolytic effects comes from the DPAG region of the brain, at least in rats. The DPAG are of the brain is thought to deal with fear-like defensive behavior via NMDA and glycine B receptors. These excitatory glutamate receptors work with the inhibitory GABA receptors to achieve equilibrium in the brain.
AP-7 has been known to cause muscle rigidity and catalepsy in rats following bilateral microinjections (0.02-0.5 nmol) into the globus pallidus and ventral-posterior portions of the caudate-putamen.
A form of AP-7, D-(-)-2-amino-7-phosphonoheptanoic acid , has also been researched. In groups of hypoxia-treated rats, D-AP7 enhanced motility, exhibited anxiogenic-like effect and impaired consolidation in passive avoidance. Both AP-7 and D-AP7 function as potent, specific antagonists of the NMDA receptor.
AP-7 functions specifically as a NMDA recognition site blocker, in contrast with 7c-KYNA which acts as a glycine site modulation blocker.
ABBREVIATIONS
AP-7 2-amino-7-phosphonoheptanoate (a NMDA recognition site blocker)
7-cKYNA, 7-chlorokynurenate (an NMDA glycine site antagonist)
See also
References
- Meldrum B, Millan M, Patel S, de Sarro G. Anti-epileptic effects of focal micro-injection of excitatory amino acid antagonists. Journal of Neural Transmission. 1988;72(3):191-200. PMID 3047315
2. “Anxiolytic effect in the elevated plus-maze of the NMDA receptor antagonist AP7 microinjected into the dorsal periaqueductal grey.” Guimarães FS, Carobrez AP, De Aguiar JC, Graeff FG. Department of Pharmacology, FMRP, University of São Paulo, Ribeirão Preto, Brazil. Psychopharmacology (Berl). 1991;103(1):91-4. PMID: 1672463 http://www.ncbi.nlm.nih.gov/pubmed/1672463
3. “Modulation of defensive behavior by periaqueductal gray NMDA/glycine-B receptor.” Carobrez AP, Teixeira KV, Graeff FG. Departamento de Farmacologia/CCB, Universidade Federal de Santa Catarina, SC 88040-900, Florianópolis, Brazil. adepadua@farmaco.ufsc.br Neurosci Biobehav Rev. 2001 Dec;25(7-8):697-709. PMID: 11801295 http://www.ncbi.nlm.nih.gov/pubmed/11801295
4. “The effect of baclofen and AP-7 on selected behavior in rats.” Car H, Wiśniewski K. Department of Pharmacology, Medical Academy in Białystok, Poland. Pharmacol Biochem Behav. 1998 Mar;59(3):685-9. PMID: 9512072 http://www.ncbi.nlm.nih.gov/pubmed/9512072
5. “Blockade of excitatory neurotransmission in the globus pallidus induces rigidity and akinesia in the rat: implications for excitatory neurotransmission in pathogenesis of Parkinson's diseases.” Turski L, Klockgether T, Turski WA, Schwarz M, Sontag KH Max-Planck Institute for Experimental Medicine, Göttingen, F.R.G. Brain Research Type: Journal Article, Research Support, Non-U.S. Gov't DOI: 10.1016/0006-8993(90)91180-O http://ukpmc.ac.uk/abstract/MED/2159826/reload=0;jsessionid=XgXmGdR8IOBFiuG26uSS.2 http://www.sciencedirect.com/science/article/pii/000689939091180O
6. “Behavioral effects of D-AP7 in rats subjected to experimental hypoxia.” Nadlewska A, Car H, Wiśniewska R, Hoły Z, Wiśniewski K. Department of Pharmacology, Medical Academy, Mickiewicza 2c, PL 15-222 Białystok, Poland. Pol J Pharmacol. 2003 May-Jun;55(3):337-44. PMID: 14506312 http://www.ncbi.nlm.nih.gov/pubmed/14506312
7. “Quinolinic acid, the inescapable neurotoxin.” Guillemin GJ. Department of Pharmacology, School of Medical Sciences, University of New South Wales, Sydney, NSW, Australia. g.guillemin@unsw.edu.au FEBS J. 2012 Apr;279(8):1356-65. doi: 10.1111/j.1742-4658.2012.08485.x. Epub 2012 Mar 27.
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