ピムアバンセリン

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Warning

• 危険有害性情報

  H315：皮膚刺激

  H319：強い眼刺激

  H335：呼吸器への刺激のおそれ

• 注意書き

  P261：粉じん/煙/ガス/ミスト/蒸気/スプレーの吸入を避ける こと。

  P264：取扱い後は皮膚をよく洗うこと。

  P264：取扱い後は手や顔をよく洗うこと。

  P271：屋外または換気の良い場所でのみ使用すること。

  P280：保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。

  P302+P352：皮膚に付着した場合：多量の水と石鹸で洗うこと。

  P304+P340：吸入した場合：空気の新鮮な場所に移し、呼吸しやすい 姿勢で休息させること。

  P305+P351+P338：眼に入った場合：水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。

  P312：気分が悪い時は医師に連絡すること。

  P321：特別な処置が必要である（このラベルの．．． を見よ）。

  P332+P313：皮膚刺激が生じた場合：医師の診断/手当てを受けるこ と。

  P337+P313：眼の刺激が続く場合：医師の診断/手当てを受けること。

  P403+P233：換気の良い場所で保管すること。容器を密閉 しておくこと。

  P405：施錠して保管すること。

  P501：内容物/容器を．．．に廃棄すること。

ピムアバンセリン 価格

ピムアバンセリン 化学特性,用途語,生産方法

• 説明

  Pimavanserin is a kind of novel oral administrated drug for treatment of Parkinson's psychosis developed by Acadia pharmaceutical Company (US) with the trade name being Pimavanserin. In September 3rd 2014, it has been granted by the US Food and Drug Administration (FDA) for breakthrough therapy certification. Breakthrough therapy certification is created by the FDA for accelerating the development and review of new drugs for treatment of serious or life-threatening diseases.
  Currently there are about seven millions to ten million of patients of Parkinson's disease worldwide with China contributing 2.6 million, ranking first in the world with 100,000 new patients emerging every year. More than 50% of patients of Parkinson's disease have had psychiatric symptoms (PDP). These psychiatric symptoms are mainly manifested as hallucinations and delusions, bringing greater challenge to the treatment and care for patients of Parkinson's disease. Dopamine is the primary target for the treatment of Parkinson's disease because most antipsychotics drugs will block the dopamine in the brain of the patients of Parkinson’s disease, making their situation of motor dysfunction be even worse, and thus currently not being suitable for these patients.
  

• 化学的特性

  Yellow Solid

• 定義

  ChEBI: Pimavanserin is a member of the class of ureas in which three of the four hydrogens are replaced by 4-fluorobenzyl, 1-methylpiperidin-4-yl, and 4-(isopropyloxy)benzyl groups. An atypical antipsychotic that is used (in the form of its tartrate salt) for treatment of hallucinations and delusions associated with Parkinson's disease. It has a role as an antipsychotic agent, a 5-hydroxytryptamine 2A receptor inverse agonist and a serotonergic antagonist. It is a member of ureas, a member of piperidines, a member of monofluorobenzenes, an aromatic ether and a tertiary amino compound. It is a conjugate base of a pimavanserin(1+).

• 生物活性

  Pimavanserin is an inverse agonist of the serotonin (5-HT) receptor subtype 5-HT_2A (IC₅₀ = 1.86 nM; K_i = 0.5 nM). It is selective for 5-HT_2A over a panel of 65 ion channels, enzymes, and receptors (K_is = >100 nM). Pimavanserin reduces head-twitch behavior and prepulse inhibition deficits induced by the 5-HT_2A receptor agonist DOI in rats at doses of 3 mg/kg, p.o. and 1-10 mg/kg, s.c., respectively. It also exhibits antipsychotic-like activity, reducing hyperactivity induced by (+)-MK-801 in mice. Pimavanserin acts synergistically with haloperidol or risperidone to suppress (+)-MK-801-induced hyperactivity and attenuates haloperidol- and risperidone-induced catalepsy in rats. Formulations containing pimavanserin have been used for the treatment of psychosis in Parkinson''s disease.

• 酵素阻害剤

  This orally active atypical non-dopaminergic antipsychotic[ (FWfree-base = 427.56 g/mol; CAS 706779-91-1 (free base) and 706782-28-7 (tartrate salt)), also known as ACP-103, Nuplazid and N-(4-fluorophenylmethyl)- N-(1-methyl-piperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenyl-methyl)carbamide, is a potent inverse agonist and antagonist at serotonin 5-HT2A receptors (Ki = 0.087 nM) and less so at serotonin 5-HT2C receptors (Ki = 0.44 nM). Pimavanserin shows low binding to σ1 receptors (Ki = 120 nM), with no appreciable affinity (Ki > 300 nM) to serotonin 5-HT2B, dopaminergic (including D2), muscarinic, histaminergic, or adrenergic receptors, or to calcium channels. 5-HT2A receptor dysregulation is implicated in both the etiology and treatment of schizophrenia, and the same receptor plays an active role in the regulation of sleep architecture. Nuplazid is specifically indicated in its FDA approval (April, 2016) for the treatment of hallucinations and delusions associated with Parkinson disease. Significantly, 5-HT2A serotonin receptor antagonists differentially regulate 5-HT2A receptor protein level in vivo. See also Ketanserin; RH-34; Risperidone; Ritanserin; Setoperone; Volinanserin.

• Mode of action

  The mechanism of action of pimavanserin in the treatment of hallucinations and delusions associated with Parkinson’s disease psychosis is unknown. However, the effect of pimavanserin could be mediated through a combination of inverse agonist and antagonist activity at serotonin 5-HT2A receptors and to a lesser extent at serotonin 5-HT2C receptors.
  www.accessdata.fda.gov

ピムアバンセリン 生産企業

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ピムアバンセリン スペクトルデータ(¹HNMR)

706779-91-1, ピムアバンセリン キーワード