AMG-9810とは？わかりやすく解説

AMG-9810
識別子
	IUPAC名 (E)-3-(4-tert-butylphenyl)-N-(2,3-dihydro-1,4-benzodioxin-6-yl)prop-2-enamide ;
CAS登録番号	545395-94-6;
PubChem; CID	680502;
ChemSpider	592741;
UNII	182HIJ2D7F;
ChEBI	CHEBI:92757;
ChEMBL	ChEMBL195789;
CompTox; Dashboard; (EPA)	DTXSID40202960 ;
ECHA InfoCard	100.164.996
化学的および物理的データ
化学式	C21H23NO3
分子量	337.419 g·mol−1
3D model; (JSmol)	Interactive image;
	SMILES CC(C)(C)C1=CC=C(C=C1)/C=C/C(=O)NC2=CC3=C(C=C2)OCCO3 ;
	InChI InChI=1S/C21H23NO3/c1-21(2,3)16-7-4-15(5-8-16)6-11-20(23)22-17-9-10-18-19(14-17)25-13-12-24-18/h4-11,14H,12-13H2,1-3H3,(H,22,23)/b11-6+ ; Key:GZTFUVZVLYUPRG-IZZDOVSWSA-N ;
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AMG-9810は、TRPV1受容体に対する強力かつ選択的なアンタゴニストとして作用する薬物である^[1]。鎮痛作用と抗炎症作用を持ち、科学研究用に使用されるが、医療用には開発されていない。高いアンタゴニストとしての作用と良好なバイオアベイラビリティと薬物動態を持つため、脳内などの疼痛知覚以外の領域におけるTRPV1の役割を研究するために使用されている^[2]^[3]^[4]^[5]^[6]。

脚注

^ “Discovery of potent, orally available vanilloid receptor-1 antagonists. Structure-activity relationship of N-aryl cinnamides”. Journal of Medicinal Chemistry 48 (1): 71–90. (January 2005). doi:10.1021/jm049485i. PMID 15634002.
^ “Transient inflammation-induced ongoing pain is driven by TRPV1 sensitive afferents”. Molecular Pain 7: 1744-8069-7-4. (January 2011). doi:10.1186/1744-8069-7-4. PMC 3025866. PMID 21219650.
^ “Involvement of central TRPV1 receptors in pentylenetetrazole and amygdala-induced kindling in male rats”. Neurological Sciences 35 (8): 1235–41. (August 2014). doi:10.1007/s10072-014-1689-5. PMID 24577898.
^ “The effect of intra-ventral hippocampus administration of TRPV1 agonist and antagonist on spatial learning and memory in male rats”. Pharmacological Reports 66 (1): 10–4. (February 2014). doi:10.1016/j.pharep.2013.06.002. PMID 24905300.
^ “Neuroinflammatory contributions to pain after SCI: roles for central glial mechanisms and nociceptor-mediated host defense”. Experimental Neurology 258: 48–61. (August 2014). doi:10.1016/j.expneurol.2014.02.001. PMID 25017887.
^ “The role of transient receptor potential vanilloid type 1 in unimodal and multimodal object recognition task in rats”. Pharmacological Reports 69 (3): 526–531. (May 2017). doi:10.1016/j.pharep.2017.01.025. PMID 31994094.

[1] “Discovery of potent, orally available vanilloid receptor-1 antagonists. Structure-activity relationship of N-aryl cinnamides”. Journal of Medicinal Chemistry 48 (1): 71–90. (January 2005). doi:10.1021/jm049485i. PMID 15634002.

[2] “Transient inflammation-induced ongoing pain is driven by TRPV1 sensitive afferents”. Molecular Pain 7: 1744-8069-7-4. (January 2011). doi:10.1186/1744-8069-7-4. PMC 3025866. PMID 21219650.

[3] “Involvement of central TRPV1 receptors in pentylenetetrazole and amygdala-induced kindling in male rats”. Neurological Sciences 35 (8): 1235–41. (August 2014). doi:10.1007/s10072-014-1689-5. PMID 24577898.

[4] “The effect of intra-ventral hippocampus administration of TRPV1 agonist and antagonist on spatial learning and memory in male rats”. Pharmacological Reports 66 (1): 10–4. (February 2014). doi:10.1016/j.pharep.2013.06.002. PMID 24905300.

[5] “Neuroinflammatory contributions to pain after SCI: roles for central glial mechanisms and nociceptor-mediated host defense”. Experimental Neurology 258: 48–61. (August 2014). doi:10.1016/j.expneurol.2014.02.001. PMID 25017887.

[6] “The role of transient receptor potential vanilloid type 1 in unimodal and multimodal object recognition task in rats”. Pharmacological Reports 69 (3): 526–531. (May 2017). doi:10.1016/j.pharep.2017.01.025. PMID 31994094.

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識別子

IUPAC名 (E)-3-(4-tert-butylphenyl)-N-(2,3-dihydro-1,4-benzodioxin-6-yl)prop-2-enamide
CAS登録番号	545395-94-6
PubChem CID	680502
ChemSpider	592741
UNII	182HIJ2D7F
ChEBI	CHEBI:92757
ChEMBL	ChEMBL195789
CompTox Dashboard (EPA)	DTXSID40202960
ECHA InfoCard	100.164.996
化学的および物理的データ
化学式	C₂₁H₂₃NO₃
分子量	337.419 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES CC(C)(C)C1=CC=C(C=C1)/C=C/C(=O)NC2=CC3=C(C=C2)OCCO3
InChI InChI=1S/C21H23NO3/c1-21(2,3)16-7-4-15(5-8-16)6-11-20(23)22-17-9-10-18-19(14-17)25-13-12-24-18/h4-11,14H,12-13H2,1-3H3,(H,22,23)/b11-6+ Key:GZTFUVZVLYUPRG-IZZDOVSWSA-N
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AMG-9810とは？ わかりやすく解説

AMG-9810

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脚注

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AMG-9810とは？わかりやすく解説