AP5 (original) (raw)
2-Amino-5-phosphonovaleriansäure (kurz APV oder AP5) ist eine synthetische, nichtproteinogene Aminosäure. APV ist ein selektiver NMDA-Rezeptor-Antagonist, das diesen Rezeptor schon in kleinen Dosen kompetitiv hemmt. Dabei wird das D-Enantiomer dieser Aminosäure als das biologisch aktive Isomer angesehen. APV wurde von und entwickelt.
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| dbo:abstract | AP5 nebo APV (2-amino-5-fosfonovalerát) je selektivní NMDA receptor, který kompetitivně inhibuje ligand (glutamát) na vazebné místě NMDA receptorů. AP5 blokuje NMDA receptory již v mikromolárních koncentracích (~50 µM). AP5 blokuje buněčný analog podmíněné reflexy u mořského plže Aplysia californica, a má účinky dlouhodobé potenciace (LTP), jelikož NMDA receptory jsou nutné pro oba procesy. Proto je někdy používán ve spojení s vápníkovým chelatem BAPTA pro určení, zda NMDARs jsou potřebné pro konkrétní buněčný proces. AP5/APV byla použita také pro studium NMDAR-dependentní LTP v savčím hypokampu. AP5 je velmi rychle působící v rámci in vitro přípravy, a může blokovat NMDA receptor v poměrně malé koncentraci. Aktivní izomer AP5 má obvykle D - konfiguraci, i když mnohé přípravky jsou k dispozici jako racemická směs D- anebo L-izomery. Pomáhá izolovat působení jiných glutamátových receptory v mozku, např. AMPA a kainátové receptory. AP5 byl vyvinut Jeffem Watkinsem a Harrym Olvermanem. (cs) AP5 (also known as APV, (2R)-amino-5-phosphonovaleric acid, or (2R)-amino-5-phosphonopentanoate) is a chemical compound used as a biochemical tool to study various cellular processes. It is a selective NMDA receptor antagonist that competitively inhibits the ligand (glutamate) binding site of NMDA receptors. AP5 blocks NMDA receptors in micromolar concentrations (~50 μM). AP5 blocks the cellular analog of classical conditioning in the sea slug Aplysia californica, and has similar effects on Aplysia long-term potentiation (LTP), since NMDA receptors are required for both. It is sometimes used in conjunction with the calcium chelator BAPTA to determine whether NMDARs are required for a particular cellular process. AP5/APV has also been used to study NMDAR-dependent LTP in the mammalian hippocampus. In general, AP5 is very fast-acting within in vitro preparations, and can block NMDA receptor action at a reasonably small concentration. The active isomer of AP5 is considered to be the D configuration, although many preparations are available as a racemic mixture of D- and L-isomers. It is useful to isolate the action of other glutamate receptors in the brain, i.e., AMPA and kainate receptors. AP5 can block the conversion of a silent synapse to an active one, since this conversion is NMDA receptor-dependent. (en) 2-Amino-5-phosphonovaleriansäure (kurz APV oder AP5) ist eine synthetische, nichtproteinogene Aminosäure. APV ist ein selektiver NMDA-Rezeptor-Antagonist, das diesen Rezeptor schon in kleinen Dosen kompetitiv hemmt. Dabei wird das D-Enantiomer dieser Aminosäure als das biologisch aktive Isomer angesehen. APV wurde von und entwickelt. (de) ácido 2-Amino-5-fosfonovaleriánico (abreviado APV o AP5) es un aminoácido no proteínico sintético. APV es un antagonista selectivo del receptor NMDA, inhibe competitivamente aún a pequeñas dosis, es decir es un antagonista competitivo. Así se puede considerar el enantiómero D-de ese aminoácido el isómero activo. APV fue desarrollado por y . (es) L'acide 2-amino-5-phosphonovalérique, parfois abrégé en APV (ou AP5) est un antagoniste sélectif des récepteurs NMDA qui inhibe par compétition le site actif de ces récepteurs. Son nom en nomenclature IUPAC est l'acide 2-amino-5-phosphonopentanoïque. Cette section ou cet article est une traduction incomplète (juillet 2017). Vous pouvez modifier la page pour effectuer la traduction. Portion de texte anglais à traduire en français Texte anglais à traduire :APV blocks the cellular analog of in the Aplysia californica, and has similar effects on Aplysia , since NMDA receptors are required for both. It is sometimes used in conjunction with the calcium to determine whether NMDARs are required for a particular cellular process. APV is generally very fast acting within in vitro preparations, and can block NMDA receptor action at a reasonably small dose. The active of APV is considered to be the D configuration, although many preparations are available as a mixture of D- and L-isomers. It is useful to isolate the action of other glutamate receptors in the brain, i.e. AMPA and kainate receptors. APV can block the conversion of a to an active one, since this conversion is NMDA receptor-dependent. APV was developed by and . Traduire ce texte • Outils • (+) (fr) D-(-)-2-アミノ-5-ホスホノペンタン酸（D-(-)-2-amino-5-phosphonopentanoic acid）は、神経細胞受容体のNMDA受容体を選択的に阻害するアンタゴニスト。D-AP5と略称される。D-(-)-2-アミノ-5-ホスホノ吉草酸（D-(-)-2-amino-5-phosphonovaleric acid、D-APV）とも呼ばれる。分子式はC5H12NO5Pであらわされ、分子量は197.13、CAS登録番号79055-68-8。光学異性体であるL-AP5よりも阻害にかかわる選択性が高いとされている。水溶性。 (ja) |
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| rdfs:comment | 2-Amino-5-phosphonovaleriansäure (kurz APV oder AP5) ist eine synthetische, nichtproteinogene Aminosäure. APV ist ein selektiver NMDA-Rezeptor-Antagonist, das diesen Rezeptor schon in kleinen Dosen kompetitiv hemmt. Dabei wird das D-Enantiomer dieser Aminosäure als das biologisch aktive Isomer angesehen. APV wurde von und entwickelt. (de) ácido 2-Amino-5-fosfonovaleriánico (abreviado APV o AP5) es un aminoácido no proteínico sintético. APV es un antagonista selectivo del receptor NMDA, inhibe competitivamente aún a pequeñas dosis, es decir es un antagonista competitivo. Así se puede considerar el enantiómero D-de ese aminoácido el isómero activo. APV fue desarrollado por y . (es) D-(-)-2-アミノ-5-ホスホノペンタン酸（D-(-)-2-amino-5-phosphonopentanoic acid）は、神経細胞受容体のNMDA受容体を選択的に阻害するアンタゴニスト。D-AP5と略称される。D-(-)-2-アミノ-5-ホスホノ吉草酸（D-(-)-2-amino-5-phosphonovaleric acid、D-APV）とも呼ばれる。分子式はC5H12NO5Pであらわされ、分子量は197.13、CAS登録番号79055-68-8。光学異性体であるL-AP5よりも阻害にかかわる選択性が高いとされている。水溶性。 (ja) AP5 nebo APV (2-amino-5-fosfonovalerát) je selektivní NMDA receptor, který kompetitivně inhibuje ligand (glutamát) na vazebné místě NMDA receptorů. AP5 blokuje NMDA receptory již v mikromolárních koncentracích (~50 µM). AP5 je velmi rychle působící v rámci in vitro přípravy, a může blokovat NMDA receptor v poměrně malé koncentraci. Aktivní izomer AP5 má obvykle D - konfiguraci, i když mnohé přípravky jsou k dispozici jako racemická směs D- anebo L-izomery. Pomáhá izolovat působení jiných glutamátových receptory v mozku, např. AMPA a kainátové receptory. (cs) AP5 (also known as APV, (2R)-amino-5-phosphonovaleric acid, or (2R)-amino-5-phosphonopentanoate) is a chemical compound used as a biochemical tool to study various cellular processes. It is a selective NMDA receptor antagonist that competitively inhibits the ligand (glutamate) binding site of NMDA receptors. AP5 blocks NMDA receptors in micromolar concentrations (~50 μM). AP5 can block the conversion of a silent synapse to an active one, since this conversion is NMDA receptor-dependent. (en) L'acide 2-amino-5-phosphonovalérique, parfois abrégé en APV (ou AP5) est un antagoniste sélectif des récepteurs NMDA qui inhibe par compétition le site actif de ces récepteurs. Son nom en nomenclature IUPAC est l'acide 2-amino-5-phosphonopentanoïque. Cette section ou cet article est une traduction incomplète (juillet 2017). Vous pouvez modifier la page pour effectuer la traduction. Portion de texte anglais à traduire en français APV can block the conversion of a to an active one, since this conversion is NMDA receptor-dependent. APV was developed by and . Traduire ce texte • Outils • (+) (fr) |
| rdfs:label | AP5 (cs) 2-Amino-5-phosphonovaleriansäure (de) AP5 (en) APV (antagonista NMDAR) (es) Acide 2-amino-5-phosphonovalérique (fr) D-(-)-2-アミノ-5-ホスホノペンタン酸 (ja) |
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