Dizocilpine (original) (raw)
ジゾシルピン（英語: Dizocilpine）は、MK-801としても知られる、水溶性の非競合的NMDA受容体アンタゴニストである。研究用試薬としてマレイン酸塩が市販されている。習慣性が示唆されているが、精神作用物質としての法規制はされていない。
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|---|---|
| dbo:abstract | Dizocilpin (INN), známý také jako MK-801, je nekompetivní antagonista NMDA receptoru, objevený ve firmě Merck v roce 1982. Glutamát je v mozku je primární excitační neurotransmiter. Kanál je normálně blokován hořečnatými ionty a vyžaduje depolarizaci neuronu a odplavení hořčíku a přístup glutamátu k otevření kanálu, což způsobí příliv vápníku, který pak vede k následné depolarizaci. Dizocilpin se váže uvnitř iontového kanálu tohoto receptoru na několik vazebných míst PCP a tím brání toku iontů, včetně vápníku (Ca2+), přes kanál. Dizocilpin blokuje NMDA receptory v použití včetně napěťového řízení. Látka působí jako silný protikřečový a pravděpodobně má vlastnosti disociativního anestetika, není používán klinicky vzhledem k objevu Olneyovy mozkové léze u laboratorních krys. Dizocilpin je také spojen s řadou negativních vedlejších účinků, včetně kognitivní poruchy a psychotických reakcí. Také inhibuje indukci dlouhodobé potenciace. V humánní medicíně se jako disociativní anestetikum místo dizocilpinu užívá ketamin. Ketamin sice také může vyvolat dočasné psychózy u některých jedinců, ale jeho krátký poločas a nižší potence přinášejí mnohem bezpečnější spektrum užití. Dizocilpin je nejčastěji používán ve zvířecích modelech pro model psychózy . Dizocilpin působí dále jako antagonista nikotinových acetylcholinových receptorů. váže a inhibuje serotoninové a dopaminové transportéry. (cs) Dizocilpine (INN), also known as MK-801, is a pore blocker of the N-Methyl-D-aspartate (NMDA) receptor, a glutamate receptor, discovered by a team at Merck in 1982. Glutamate is the brain's primary excitatory neurotransmitter. The channel is normally blocked with a magnesium ion and requires depolarization of the neuron to remove the magnesium and allow the glutamate to open the channel, causing an influx of calcium, which then leads to subsequent depolarization. Dizocilpine binds inside the ion channel of the receptor at several of PCP's binding sites thus preventing the flow of ions, including calcium (Ca2+), through the channel. Dizocilpine blocks NMDA receptors in a use- and voltage-dependent manner, since the channel must open for the drug to bind inside it. The drug acts as a potent anti-convulsant and probably has dissociative anesthetic properties, but it is not used clinically for this purpose because of the discovery of brain lesions, called Olney's lesions (see below), in laboratory rats. Dizocilpine is also associated with a number of negative side effects, including cognitive disruption and psychotic-spectrum reactions. It inhibits the induction of long term potentiation and has been found to impair the acquisition of difficult, but not easy, learning tasks in rats and primates. Because of these effects of dizocilpine, the NMDA receptor pore blocker ketamine is used instead as a dissociative anesthetic in human medical procedures. While ketamine may also trigger temporary psychosis in certain individuals, its short half-life and lower potency make it a much safer clinical option. However, dizocilpine is the most frequently used uncompetitive NMDA receptor antagonist in animal models to mimic psychosis for experimental purposes. Dizocilpine has also been found to act as a nicotinic acetylcholine receptor antagonist. It has been shown to bind to and inhibit the serotonin and dopamine transporters as well. (en) ジゾシルピン（英語: Dizocilpine）は、MK-801としても知られる、水溶性の非競合的NMDA受容体アンタゴニストである。研究用試薬としてマレイン酸塩が市販されている。習慣性が示唆されているが、精神作用物質としての法規制はされていない。 (ja) Dizocylpina (łac. Dizolcipinum) – bardzo silny antagonista niewspółzawodniczący receptora NMDA, używany sporadycznie jako lek przeciwdrgawkowy. (pl) |
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| rdfs:comment | ジゾシルピン（英語: Dizocilpine）は、MK-801としても知られる、水溶性の非競合的NMDA受容体アンタゴニストである。研究用試薬としてマレイン酸塩が市販されている。習慣性が示唆されているが、精神作用物質としての法規制はされていない。 (ja) Dizocylpina (łac. Dizolcipinum) – bardzo silny antagonista niewspółzawodniczący receptora NMDA, używany sporadycznie jako lek przeciwdrgawkowy. (pl) Dizocilpin (INN), známý také jako MK-801, je nekompetivní antagonista NMDA receptoru, objevený ve firmě Merck v roce 1982. Glutamát je v mozku je primární excitační neurotransmiter. Kanál je normálně blokován hořečnatými ionty a vyžaduje depolarizaci neuronu a odplavení hořčíku a přístup glutamátu k otevření kanálu, což způsobí příliv vápníku, který pak vede k následné depolarizaci. Dizocilpin se váže uvnitř iontového kanálu tohoto receptoru na několik vazebných míst PCP a tím brání toku iontů, včetně vápníku (Ca2+), přes kanál. Dizocilpin blokuje NMDA receptory v použití včetně napěťového řízení. Látka působí jako silný protikřečový a pravděpodobně má vlastnosti disociativního anestetika, není používán klinicky vzhledem k objevu Olneyovy mozkové léze u laboratorních krys. Dizocilpin je (cs) Dizocilpine (INN), also known as MK-801, is a pore blocker of the N-Methyl-D-aspartate (NMDA) receptor, a glutamate receptor, discovered by a team at Merck in 1982. Glutamate is the brain's primary excitatory neurotransmitter. The channel is normally blocked with a magnesium ion and requires depolarization of the neuron to remove the magnesium and allow the glutamate to open the channel, causing an influx of calcium, which then leads to subsequent depolarization. Dizocilpine binds inside the ion channel of the receptor at several of PCP's binding sites thus preventing the flow of ions, including calcium (Ca2+), through the channel. Dizocilpine blocks NMDA receptors in a use- and voltage-dependent manner, since the channel must open for the drug to bind inside it. The drug acts as a potent (en) |
| rdfs:label | Dizocilpin (cs) Dizocilpine (en) ジゾシルピン (ja) Dizocylpina (pl) |
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