israpafantとは？わかりやすく解説

イスラパファント
法的地位
法的地位	US: Investigational New Drug;
識別子
	IUPAC名 (6R)-4-(2-Chlorophenyl)-2-[2-(4-isobutylphenyl)ethyl]-6,9-dimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine ;
CAS登録番号	117279-73-9 ;
PubChem; CID	636426;
ChemSpider	552203;
UNII	O3MCV749SW;
CompTox; Dashboard; (EPA)	DTXSID001102657 ;
化学的および物理的データ
化学式	C28H29ClN4S
分子量	489.08 g·mol−1
3D model; (JSmol)	Interactive image;
	SMILES C[C@@H]1C2=NN=C(N2C3=C(C=C(S3)CCC4=CC=C(C=C4)CC(C)C)C(=N1)C5=CC=CC=C5Cl)C ;
	InChI InChI=1S/C28H29ClN4S/c1-17(2)15-21-11-9-20(10-12-21)13-14-22-16-24-26(23-7-5-6-8-25(23)29)30-18(3)27-32-31-19(4)33(27)28(24)34-22/h5-12,16-18H,13-15H2,1-4H3/t18-/m1/s1 ; Key:RMSWMRJVUJSDGN-GOSISDBHSA-N ;
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イスラパファント（英：Israpafant、Y-24180）は、血小板活性化因子受容体に対する選択的受容体拮抗薬として作用する薬物であり^[1]、本来は気管支喘息の治療のため開発された^[2]。

化学構造はチエノトリアゾロジアゼピンで、鎮静薬であるベンゾジアゼピン誘導体エチゾラムと密接な関係がある。However israpafant binds far more tightly to the platelet-activating factor receptor, with an IC₅₀ of 0.84nM for inhibiting PAF-induced human platelet aggregation (compared to etizolam's IC₅₀ of 998nM at this target), while it binds only weakly to benzodiazepine receptors, with a Ki of 3680nM.^[3] イスラパファントは好酸球の活性化を阻害することにより^[4]^[5]^[6]、免疫反応の発現を遅らせることが分かっている。また、抗腎毒性特性^[7]やカルシウム輸送の促進^[8]があることも示されている。

脚注

^ “Amino acid residues critical for endoplasmic reticulum export and trafficking of platelet-activating factor receptor”. The Journal of Biological Chemistry 285 (8): 5931–40. (February 2010). doi:10.1074/jbc.M109.066282. PMC 2820818. PMID 200077156
^ “Effects of a PAF antagonist, Y-24180, on bronchial hyperresponsiveness in patients with asthma”. American Journal of Respiratory and Critical Care Medicine 152 (4 Pt 1): 1198–202. (October 1995). doi:10.1164/ajrccm.152.4.7551370. PMID 7551370.
^ “Pharmacological actions of Y-24180, a new specific antagonist of platelet activating factor (PAF): II. Interactions with PAF and benzodiazepine receptors”. Prostaglandins 40 (6): 571–83. (December 1990). doi:10.1016/0090-6980(90)90002-D. PMID 1965554.
^ “Inhibition of activation of human peripheral blood eosinophils by Y-24180, an antagonist to platelet-activating factor receptor”. Life Sciences 65 (13): PL171-6. (1999). doi:10.1016/s0024-3205(99)00385-9. PMID 10503965.
^ “Inhibition of eosinophil activation in bronchoalveolar lavage fluid from atopic asthmatics by Y-24180, an antagonist to platelet-activating factor”. Life Sciences 65 (20): 2031–9. (1999). doi:10.1016/s0024-3205(99)00470-1. PMID 10579457.
^ “Differential effect of antiallergic drugs on IgE-mediated cutaneous reaction in passively sensitized mice”. Pharmacology 60 (2): 97–104. (February 2000). doi:10.1159/000028353. PMID 106577596
^ “Preventive effect of platelet-activating factor antagonist, Y-24180, against cyclosporine-induced acute nephrotoxicity”. Life Sciences 68 (10): 1181–90. (January 2001). doi:10.1016/s0024-3205(00)01028-6. PMID 11228102.
^ “Effect of Y-24180 on Ca2+ movement and proliferation in renal tubular cells”. Life Sciences 74 (7): 923–33. (January 2004). doi:10.1016/j.lfs.2003.09.033. PMID 14659980.

[:0-1] “Amino acid residues critical for endoplasmic reticulum export and trafficking of platelet-activating factor receptor”. The Journal of Biological Chemistry 285 (8): 5931–40. (February 2010). doi:10.1074/jbc.M109.066282. PMC 2820818. PMID 200077156

[:1-2] “Effects of a PAF antagonist, Y-24180, on bronchial hyperresponsiveness in patients with asthma”. American Journal of Respiratory and Critical Care Medicine 152 (4 Pt 1): 1198–202. (October 1995). doi:10.1164/ajrccm.152.4.7551370. PMID 7551370.

[:2-3] “Pharmacological actions of Y-24180, a new specific antagonist of platelet activating factor (PAF): II. Interactions with PAF and benzodiazepine receptors”. Prostaglandins 40 (6): 571–83. (December 1990). doi:10.1016/0090-6980(90)90002-D. PMID 1965554.

[:3-4] “Inhibition of activation of human peripheral blood eosinophils by Y-24180, an antagonist to platelet-activating factor receptor”. Life Sciences 65 (13): PL171-6. (1999). doi:10.1016/s0024-3205(99)00385-9. PMID 10503965.

[:4-5] “Inhibition of eosinophil activation in bronchoalveolar lavage fluid from atopic asthmatics by Y-24180, an antagonist to platelet-activating factor”. Life Sciences 65 (20): 2031–9. (1999). doi:10.1016/s0024-3205(99)00470-1. PMID 10579457.

[:5-6] “Differential effect of antiallergic drugs on IgE-mediated cutaneous reaction in passively sensitized mice”. Pharmacology 60 (2): 97–104. (February 2000). doi:10.1159/000028353. PMID 106577596

[:6-7] “Preventive effect of platelet-activating factor antagonist, Y-24180, against cyclosporine-induced acute nephrotoxicity”. Life Sciences 68 (10): 1181–90. (January 2001). doi:10.1016/s0024-3205(00)01028-6. PMID 11228102.

[:7-8] “Effect of Y-24180 on Ca2+ movement and proliferation in renal tubular cells”. Life Sciences 74 (7): 923–33. (January 2004). doi:10.1016/j.lfs.2003.09.033. PMID 14659980.

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israpafantとは？わかりやすく解説

イスラパファント

関連記事

脚注

英和和英テキスト翻訳

「israpafant」の関連用語

法的地位

法的地位	US: Investigational New Drug
識別子
IUPAC名 (6R)-4-(2-Chlorophenyl)-2-[2-(4-isobutylphenyl)ethyl]-6,9-dimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine
CAS登録番号	117279-73-9
PubChem CID	636426
ChemSpider	552203
UNII	O3MCV749SW
CompTox Dashboard (EPA)	DTXSID001102657
化学的および物理的データ
化学式	C₂₈H₂₉ClN₄S
分子量	489.08 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES C[C@@H]1C2=NN=C(N2C3=C(C=C(S3)CCC4=CC=C(C=C4)CC(C)C)C(=N1)C5=CC=CC=C5Cl)C
InChI InChI=1S/C28H29ClN4S/c1-17(2)15-21-11-9-20(10-12-21)13-14-22-16-24-26(23-7-5-6-8-25(23)29)30-18(3)27-32-31-19(4)33(27)28(24)34-22/h5-12,16-18H,13-15H2,1-4H3/t18-/m1/s1 Key:RMSWMRJVUJSDGN-GOSISDBHSA-N
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israpafantとは？ わかりやすく解説

イスラパファント

関連記事

脚注

急上昇のことば

英和和英テキスト翻訳

「israpafant」の関連用語

israpafantとは？わかりやすく解説