関: lobeline hydrochloride、smokeless

WordNet

emitting or containing little or no smoke; "smokeless factory stacks"; "smokeless fuel"; "a smokeless environment"

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(石炭・炉)などが)[ほとんど]煙の出ない,無煙の

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/09/23 15:46:54」(JST)

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Lobeline is a natural alkaloid found in "Indian tobacco" (Lobelia inflata), "Devil's tobacco" (Lobelia tupa), "cardinal flower" (Lobelia cardinalis), "great lobelia" (Lobelia siphilitica), and Hippobroma longiflora. Additionally, it is also found in Lobelia chinensis. In its pure form it is a white amorphous powder which is freely soluble in water.

Lobeline has been used as a smoking cessation aid,^[1]^[2]^[3] and may have application in the treatment of other drug addictions such as addiction to amphetamines,^[4]^[5] cocaine^[6] or alcohol.^[7]

Lobeline has multiple mechanisms of action, acting as a VMAT2 ligand,^[8]^[9]^[10] which stimulates dopamine release to a moderate extent when administered alone, but reduces the dopamine release caused by methamphetamine.^[11]^[12] It also inhibits the reuptake of dopamine and serotonin,^[13] and acts as a mixed agonist–antagonist at nicotinic acetylcholine receptors ^[14]^[15] to which it binds at the subunit interfaces of the extracellular domain. ^[16] and an antagonist at μ-opioid receptors.^[17]

References

^ Stead LF, Hughes JR (2012). "Lobeline for smoking cessation". Cochrane Database Syst Rev 2: CD000124. doi:10.1002/14651858.CD000124.pub2. PMID 22336780.
^ Marlow SP, Stoller JK. Smoking cessation. Respiratory Care. 2003 Dec;48(12):1238-56. PMID 14651764
^ Buchhalter AR, Fant RV, Henningfield JE. Novel pharmacological approaches for treating tobacco dependence and withdrawal : current status. Drugs. 2008;68(8):1067-88. PMID 18484799
^ Neugebauer NM, Harrod SB, Stairs DJ, Crooks PA, Dwoskin LP, Bardo MT. Lobelane decreases methamphetamine self-administration in rats. European Journal of Pharmacology. 2007 Sep 24;571(1):33-8. doi:10.1016/j.ejphar.2007.06.003 PMID 17612524
^ Eyerman DJ, Yamamoto BK. Lobeline attenuates methamphetamine-induced changes in vesicular monoamine transporter 2 immunoreactivity and monoamine depletions in the striatum. Journal of Pharmacology and Experimental Therapeutics. 2005 Jan;312(1):160-9. PMID 15331654
^ Polston JE, Cunningham CS, Rodvelt KR, Miller DK. Lobeline augments and inhibits cocaine-induced hyperactivity in rats. Life Sciences. 2006 Aug 1;79(10):981-90. PMID 16765386
^ Farook JM, Lewis B, Gaddis JG, Littleton JM, Barron S. Lobeline, a nicotinic partial agonist attenuates alcohol consumption and preference in male C57BL/6J mice. Physiology and Behavior. 2009 Jun 22;97(3-4):503-6. PMID 19268674
^ Zheng G, Dwoskin LP, Crooks PA. Vesicular monoamine transporter 2: role as a novel target for drug development. AAPS Journal. 2006 Nov 10;8(4):E682-92. doi:10.1208/aapsj080478 PMID 17233532
^ Zheng F, Zheng G, Deaciuc AG, Zhan CG, Dwoskin LP, Crooks PA. Computational neural network analysis of the affinity of lobeline and tetrabenazine analogs for the vesicular monoamine transporter-2. Bioorganic and Medicinal Chemistry. 2007 Apr 15;15(8):2975-92. PMID 17331733
^ Zheng G, Dwoskin LP, Deaciuc AG, Norrholm SD, Crooks PA. Defunctionalized lobeline analogues: structure-activity of novel ligands for the vesicular monoamine transporter. Journal of Medicinal Chemistry. 2005 Aug 25;48(17):5551-60. PMID 16107155
^ Wilhelm CJ, Johnson RA, Eshleman AJ, Janowsky A. Lobeline effects on tonic and methamphetamine-induced dopamine release. Biochemical Pharmacology. 2008 Mar 15;75(6):1411-5. PMID 18191815
^ Wilhelm CJ, Johnson RA, Lysko PG, Eshleman AJ, Janowsky A. Effects of methamphetamine and lobeline on vesicular monoamine and dopamine transporter-mediated dopamine release in a cotransfected model system. Journal of Pharmacology and Experimental Therapeutics. 2004 Sep;310(3):1142-51. PMID 15102929
^ Zheng G, Horton DB, Deaciuc AG, Dwoskin LP, Crooks PA. Des-keto lobeline analogs with increased potency and selectivity at dopamine and serotonin transporters. Bioorganic and Medicinal Chemistry Letters. 2006 Oct 1;16(19):5018-21. PMID 16905316
^ Damaj MI, Patrick GS, Creasy KR, Martin BR. Pharmacology of lobeline, a nicotinic receptor ligand. Journal of Pharmacology and Experimental Therapeutics. 1997 Jul;282(1):410-9. PMID 9223582
^ Miller DK, Harrod SB, Green TA, Wong MY, Bardo MT, Dwoskin LP. Lobeline attenuates locomotor stimulation induced by repeated nicotine administration in rats. Pharmacology, Biochemistry and Behaviour. 2003 Jan;74(2):279-86. PMID 12479946
^ PDB entry 2bys. Hansen et al. Structures of Aplysia Achbp Complexes with Nicotinic Agonists and Antagonists Reveal Distinctive Binding Interfaces and Conformations. 'EMBO J. 2005 24:23653-91. PMID 16193063
^ Miller DK, Lever JR, Rodvelt KR, Baskett JA, Will MJ, Kracke GR. Lobeline, a potential pharmacotherapy for drug addiction, binds to mu opioid receptors and diminishes the effects of opioid receptor agonists. Drug and Alcohol Dependence. 2007 Jul 10;89(2-3):282-91. PMID 17368966

English Journal

Nicotine effects on human endothelial intercellular communication via α4β2 and α3β2 nicotinic acetylcholine receptor subtypes.

Duerrschmidt N, Hagen A, Gaertner C, Wermke A, Nowicki M, Spanel-Borowski K, Stepan H, Mohr FW, Dhein S.SourceClinic for Cardiac Surgery, Heart Centre, University of Leipzig, Strümpellstr. 39, 04289, Leipzig, Germany.
Naunyn-Schmiedeberg's archives of pharmacology.Naunyn Schmiedebergs Arch Pharmacol.2012 Feb 22. [Epub ahead of print]
Since previous in vitro experiments revealed that nicotine can impair endothelial intercellular communication via the downregulation of connexin43 (Cx43), we wanted to find out which nicotinic acetylcholine receptors are involved in the molecular mechanism of communication failure. Cultured human en
PMID 22349182

Lobeline for smoking cessation.

Stead LF, Hughes JR.SourceDepartment of Primary Care Health Sciences, University of Oxford, 23-38 Hythe Bridge Street, Oxford, UK, OX1 2ET.
Cochrane database of systematic reviews (Online).Cochrane Database Syst Rev.2012 Feb 15;2:CD000124.
BACKGROUND: Lobeline is a partial nicotine agonist, which has been used in a variety of commercially available preparations to help stop smoking.OBJECTIVES: The objective of this review was to assess the effects of lobeline on long term smoking cessation.SEARCH METHODS: We searched the Cochrane Toba
PMID 22336780

Enhanced meta-analysis of acetylcholine binding protein structures reveals conformational signatures of agonism in nicotinic receptors.

Stober ST, Abrams CF.SourceDepartment of Chemical and Biological Engineering, Drexel University, 3141 Chestnut St., Philadelphia, PA 19104.
Protein science : a publication of the Protein Society.Protein Sci.2011 Dec 14. doi: 10.1002/pro.2016. [Epub ahead of print]
The soluble acetylcholine binding protein (AChBP) is the default structural proxy for pentameric ligand-gated ion channel (LGICs). Unfortunately, it is difficult to recognize conformational signatures of LGIC agonism and antagonism within the large set of AChBP crystal structures in both apo and lig
PMID 22170867

Japanese Journal

シビレエイ電気器官のニコチン性アセチルコリン受容体/イオンチャンネル複合体に対するイミダクロプリドおよびその関連化合物の薬理的作用

冨澤元博,大塚博子,宮本徹,山本出
日本農薬学会誌 20(1), 49-56, 1995-02-20
シビレエイ電気器官のニコチン性アセチルコリンレセプターイオンチャンネル複合体へのイミダクロプリド関連化合物を含む各種リガンドの効果について, アセチルコリン(ACh)認識部位のプローブである[^3H]α-ブンガロトキシンおよびイオンチャンネル内のアロステリック部位のプローブである[^3H]フェンサイクリジンを用いたラジオレセプターアッセイにより検討した.ニコチン, アナバシン, カルバコールおよび …
NAID 110001712790

Growth and Lobeline Production of Lobelia inflata Hairy Roots

Ishimaru Kanji [他]
生薬学雑誌 46(3), p265-267, 1992-09
NAID 40001834740

Lobeline Production by Hairy Root Cultures of Lobelina Inflata

YONEMITSU H.
Plant Cell Rep. 9, 307-310, 1990
NAID 80005586476

Related Pictures

★リンクテーブル★

リンク元	「呼吸興奮薬」「ロベリン」「smokeless」
拡張検索	「lobeline hydrochloride」

「呼吸興奮薬」

Lobeline
Systematic (IUPAC) name
	2-((2R,6S)-6-((S)-2-Hydroxy-2-phenylethyl)-1-methylpiperidin-2-yl)-1-phenylethanone
Clinical data
AHFS/Drugs.com	International Drug Names
Legal status	?
Identifiers
CAS number	90-69-7
ATCvet code	QV04CV01
PubChem	CID 101616
ChemSpider	91814
UNII	D0P25S3P81
KEGG	D02364
ChEMBL	CHEMBL15476
Chemical data
Formula	C22H27NO2
Mol. mass	337.455
	SMILES O=C(C[C@@H]1N([C@@H](CCC1)C[C@@H](C2=CC=CC=C2)O)C)C3=CC=CC=C3;
	InChI InChI=1S/C22H27NO2/c1-23-19(15-21(24)17-9-4-2-5-10-17)13-8-14-20(23)16-22(25)18-11-6-3-7-12-18/h2-7,9-12,19-21,24H,8,13-16H2,1H3/t19-,20+,21-/m0/s1 ; Key:MXYUKLILVYORSK-HBMCJLEFSA-N ;
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