piperoxan

Piperoxan
Systematic (IUPAC) name
	1-(2,3-dihydro-1,4-benzodioxin-2-ylmethyl)piperidine
Clinical data
Legal status	Uncontrolled
Routes	Oral
Identifiers
CAS number	59-39-2; 135-87-5 (hydrochloride)
ATC code	None
PubChem	CID 6040
ChemSpider	5817
UNII	9ZCS27634Y
ChEMBL	CHEMBL31836
Chemical data
Formula	C14H19NO2
Mol. mass	233.31 g/mol
	SMILES O1c3c(OC(C1)CN2CCCCC2)cccc3;

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/02/10 20:23:26」(JST)

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Piperoxan, also known as benodaine, is a drug which was the very first antihistamine to be discovered.^[1]^[2] This compound, derived from benzodioxan, was prepared in the early 1930s by Daniel Bovet and Ernest Fourneau at the Pasteur Institute in France.^[1]^[2] Formerly investigated by Fourneau as an α-adrenergic-blocking agent, they demonstrated that it also antagonized histamine-induced bronchospasm in guinea pigs, and published their findings in 1933.^[1]^[2]^[3] Bovet went on to win the 1957 Nobel Prize in Physiology or Medicine for his contribution,^[4] and one of their students, Anne-Marie Staub, published the first structure-activity relationship (SAR) study of antihistamines in 1939.^[1]

References[edit]

^ ^a ^b ^c ^d Scriabine, Alexander; Landau, Ralph; Achilladelis, Basil (1999). Pharmaceutical innovation: revolutionizing human health. Philadelphia: Chemical Heritage Press. ISBN 0-941901-21-1.
^ ^a ^b ^c Williams, David H.; Lemke, Thomas L.; Foye, William O. (2008). Foye's principles of medicinal chemistry. Hagerstwon, MD: Lippincott Williams & Wilkins. ISBN 0-7817-6879-9.
^ Fourneau, Ernest; Bovet, Daniel (1933). "Recherches sur l'action sympathicolytique d'un nouveau dérivé du dioxane". Archives Internationales de Pharmacodynamie et de Thérapie 46: 178–91. ISSN 0003-9780. Cite uses deprecated parameters (help)
^ "Daniel Bovet - Biography".

English Journal

Chronic treatment with the α2-adrenoceptor antagonist fluparoxan prevents age-related deficits in spatial working memory in APP×PS1 transgenic mice without altering β-amyloid plaque load or astrocytosis.

Scullion GA1, Kendall DA, Marsden CA, Sunter D, Pardon MC.
Neuropharmacology.Neuropharmacology.2011 Feb-Mar;60(2-3):223-34. doi: 10.1016/j.neuropharm.2010.09.002. Epub 2010 Sep 17.
Locus coeruleus degeneration and reduced central noradrenaline content is an early feature of Alzheimer's disease. In transgenic mouse models of Alzheimer's disease-like pathology, lesioning the locus coeruleus exacerbates β-amyloid (Aβ) pathology, neuroinflammation and memory deficits. Here we ai
PMID 20850464

Role of alpha-2 adrenergic receptors in anti-ulcer effect mechanism of estrogen and luteinising hormone on rats.

Borekci B1, Kumtepe Y, Karaca M, Halici Z, Cadirci E, Albayrak F, Polat B, Suleyman H.
Gynecological endocrinology : the official journal of the International Society of Gynecological Endocrinology.Gynecol Endocrinol.2009 Apr;25(4):264-8. doi: 10.1080/09513590802630104.
OBJECTIVE: To evaluate anti-ulcer effect of estrogen and luteinising hormone (LH) on indomethacin-induced ulcer model in female rats.STUDY DESIGN: Ovariectomy in healthy adult famale rats. Acute administration of estradiol to ovariectomised rats. Acute administration of LH to intact rats. Combined a
PMID 19340627

Neurochemical interaction between dopaminergic and noradrenergic neurons in the medial prefrontal cortex.

Pan WH1, Yang SY, Lin SK.
Synapse (New York, N.Y.).Synapse.2004 Jul;53(1):44-52.
Growing evidence indicates that there is an interaction between the transmission of dopamine (DA) and norepinephrine (NE) in the noradrenergic and dopaminergic projections that converge in the medial prefrontal cortex (mPFC). The effects of the noradrenergic alpha1 and alpha2 receptors and the NE tr
PMID 15150740

Japanese Journal

Spinal .ALPHA.1- and .ALPHA.2-adrenoceptors mediate facilitation and inhibition of spinal motor transmission, respectively.

TANABE Mitsuo,ONO Hideki,FUKUDA Hideomi
The Japanese Journal of Pharmacology 54(1), 69-77, 1990
… The depression of PSR was antagonized by the α<SUB>2</SUB>-antagonist piperoxan. … These inhibitions were antagonized by piperoxan. …
NAID 130000832898