ジメモルファン

ジメモルファン
IUPAC命名法による物質名
	IUPAC名 (4bS,8aS,9S)-3,11-Dimethyl-6,7,8,8a,9,10-hexahydro-5H-9,4b-(epiminoethano)phenanthrene;
臨床データ
Drugs.com	国別販売名(英語); International Drug Names
識別
CAS番号;	36309-01-0
ATCコード	R05DA11 (WHO)
PubChem	CID: 3037918
ChemSpider	16735785
UNII	623OAC38YU
KEGG	D07848
ChEMBL	CHEMBL2106325
化学的データ
化学式	C18H25N
分子量	255.398 g/mol
	SMILES CC1=CC2=C(C[C@@H]3N(CC[C@@]42CCCC[C@H]34)C)C=C1;
	InChI InChI=1S/C18H25N/c1-13-6-7-14-12-17-15-5-3-4-8-18(15,16(14)11-13)9-10-19(17)2/h6-7,11,15,17H,3-5,8-10,12H2,1-2H3/t15-,17+,18+/m1/s1 ; Key:KBEZZLAAKIIPFK-NJAFHUGGSA-N ;

ジメモルファン (国際一般名：Dimemorfan。Dimemorphan と綴る場合もある) は、日本の他スペインやイタリアなどの各国[1][2][3][4]で広く使用されているモルフィナン系の鎮咳薬である。日本での一般名はジメモルファンリン酸塩で、山之内製薬 (現アステラス製薬) が開発し、1975年に日本で発売された。ジメモルファンはデキストロメトルファン (DXM) およびその活性代謝物であるデキストロルファン (DXO) のアナログで、これらと同様に強力な σ₁受容体アゴニストとして作用する (K_i=151 nM)[5][6]。一方、DXM や DXO と異なり、NMDA受容体アンタゴニストとしては作用せず (K_i = 16,978 nM)、このため解離を起こさないので副作用や乱用の可能性が相対的に低くなっている[7][8]。また、DXM や DXO 同様、ジメモルファンの σ₂ 受容体への親和性は比較的低い (K_i = 4,421 nM)。

参考文献

The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. (14 November 2014). pp. 427–. ISBN 978-1-4757-2085-3
Bruera, Eduardo; Higginson, Irene; von Gunten, Charles F.; Morita, Tatsuya (15 January 2015). Textbook of Palliative Medicine and Supportive Care, Second Edition. CRC Press. pp. 677–. ISBN 978-1-4441-3526-8
“The nonnarcotic antitussive drug dimemorfan: a review”. Clinical Therapeutics 19 (2): 215–31. (1997). doi:10.1016/S0149-2918(97)80111-7. PMID 9152562.
Armstrong, Lora L.; Goldman, Morton P. (1 January 2005). Lexi-Comp's Drug Information Handbook International: With Canadian and International Drug Monographs. Lexi-Comp. ISBN 978-1-59195-110-0
“The pharmacology of sigma-1 receptors”. Pharmacology & Therapeutics 124 (2): 195–206. (November 2009). doi:10.1016/j.pharmthera.2009.07.001. PMC 2785038. PMID 19619582.
Botana, Luis M.; Loza, Mabel (20 April 2012). Therapeutic Targets: Modulation, Inhibition, and Activation. John Wiley & Sons. pp. 234–. ISBN 978-1-118-18552-0
“Binding of dimemorfan to sigma-1 receptor and its anticonvulsant and locomotor effects in mice, compared with dextromethorphan and dextrorphan”. Brain Research 821 (2): 516–9. (March 1999). doi:10.1016/S0006-8993(99)01125-7. PMID 10064839.
“The dextromethorphan analog dimemorfan attenuates kainate-induced seizures via sigma1 receptor activation: comparison with the effects of dextromethorphan”. British Journal of Pharmacology 144 (7): 908–18. (April 2005). doi:10.1038/sj.bjp.0705998. PMC 1576070. PMID 15723099.

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[Elks2014-1] The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. (14 November 2014). pp. 427–. ISBN 978-1-4757-2085-3

[BrueraHigginson2015-2] Bruera, Eduardo; Higginson, Irene; von Gunten, Charles F.; Morita, Tatsuya (15 January 2015). Textbook of Palliative Medicine and Supportive Care, Second Edition. CRC Press. pp. 677–. ISBN 978-1-4441-3526-8

[Ida1997-3] “The nonnarcotic antitussive drug dimemorfan: a review”. Clinical Therapeutics 19 (2): 215–31. (1997). doi:10.1016/S0149-2918(97)80111-7. PMID 9152562.

[ArmstrongGoldman2005-4] Armstrong, Lora L.; Goldman, Morton P. (1 January 2005). Lexi-Comp's Drug Information Handbook International: With Canadian and International Drug Monographs. Lexi-Comp. ISBN 978-1-59195-110-0

[MauriceSu2009-5] “The pharmacology of sigma-1 receptors”. Pharmacology & Therapeutics 124 (2): 195–206. (November 2009). doi:10.1016/j.pharmthera.2009.07.001. PMC 2785038. PMID 19619582.

[BotanaLoza2012-6] Botana, Luis M.; Loza, Mabel (20 April 2012). Therapeutic Targets: Modulation, Inhibition, and Activation. John Wiley & Sons. pp. 234–. ISBN 978-1-118-18552-0

[ChouLiao1999-7] “Binding of dimemorfan to sigma-1 receptor and its anticonvulsant and locomotor effects in mice, compared with dextromethorphan and dextrorphan”. Brain Research 821 (2): 516–9. (March 1999). doi:10.1016/S0006-8993(99)01125-7. PMID 10064839.

[ShinNah2005-8] “The dextromethorphan analog dimemorfan attenuates kainate-induced seizures via sigma1 receptor activation: comparison with the effects of dextromethorphan”. British Journal of Pharmacology 144 (7): 908–18. (April 2005). doi:10.1038/sj.bjp.0705998. PMC 1576070. PMID 15723099.

ジメモルファン

関連項目

参考文献