関: eptazocine hydrobromide

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/05/29 06:49:06」(JST)

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Eptazocine (Sedapain) is an opioid analgesic which was introduced in Japan by Morishita in 1987.^[1]^[2]^[3]^[4] It acts as a mixed κ-opioid receptor agonist and μ-opioid receptor antagonist.^[4]^[5]^[6]

References [edit]

^ Index nominum 2000: international drug directory. Taylor & Francis US. 2000. p. 396. ISBN 978-3-88763-075-1. Retrieved 29 November 2011.
^ American Chemical Society. Division of Medicinal Chemistry (1990). Annual Reports in Medicinal Chemistry. Academic Press. p. 381. ISBN 978-0-12-040525-1. Retrieved 29 November 2011.
^ Nabeshima T, Matsuno K, Kamei H, Kameyama T (May 1985). "The interaction of eptazocine, a novel analgesic, with opioid receptors". Research Communications in Chemical Pathology and Pharmacology 48 (2): 173–81. PMID 2992058.
^ ^a ^b Hiroshi Nagase; Silvia N. Calderon (21 January 2011). Chemistry of Opioids. Springer. p. 280. ISBN 978-3-642-18106-1. Retrieved 29 November 2011.
^ Tamura T, Ogawa J, Taniguchi T, Waki I (January 1990). "[Preferential action of eptazocine, a novel analgesic, with opioid receptors in isolated guinea pig ileum and mouse vas deferens preparations]". Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica (in Japanese) 95 (1): 41–6. PMID 2154395.
^ Dr. Ian Morton; Ian K. M. Morton; Judith M. Hall; Dr. Judith Hall (1999). Concise dictionary of pharmacological agents: properties and synonyms. Springer. p. 113. ISBN 978-0-7514-0499-9. Retrieved 29 November 2011.

English Journal

Asymmetric syntheses of (-)-pentazocine and (-)-eptazocine through an aza-Prins cyclization.

Chen Q, Huo X, Yang Z, She X.SourceState Key Laboratory of Applied Organic Chemistry, Department of Chemistry, Lanzhou University, Lanzhou 730000, PR China.
Chemistry, an Asian journal.Chem Asian J.2012 Nov;7(11):2543-6. doi: 10.1002/asia.201200505. Epub 2012 Aug 21.
Two down more to go: The asymmetric syntheses of (-)-pentazocine and (-)-eptazocine are presented. The highlights of the syntheses are the construction of the core skeleton through an aza-Prins cyclization and intramolecular Friedel-Crafts reaction.Copyright © 2012 WILEY-VCH Verlag GmbH & Co. K
PMID 22907930

Investigation of transport mechanism of pentazocine across the blood-brain barrier using the in situ rat brain perfusion technique.

Suzuki T, Oshimi M, Tomono K, Hanano M, Watanabe J.SourceDepartment of Pharmaceutics, College of Pharmacy, Nihon University, 7-7-1 Narashinodai, Funabashi-shi, Chiba 274-8555, Japan. tsuzuki@pha.nihon-u.ac.jp
Journal of pharmaceutical sciences.J Pharm Sci.2002 Nov;91(11):2346-53.
To characterize pentazocine (PTZ) transport across the blood-brain barrier (BBB), the cerebrovascular permeability-surface area product (PS(inf)) of PTZ was determined by a well-established in situ rat brain perfusion technique. The uptake kinetics of PTZ by the rat brain exhibited saturability, whi
PMID 12379919

Investigation on the influx transport mechanism of pentazocine at the blood-brain barrier in rats using the carotid injection technique.

Suzuki T, Moriki Y, Goto H, Tomono K, Hanano M, Watanabe J.SourceDepartment of Pharmaceutics, College of Pharmacy, Nihon University, Funabashi, Chiba, Japan. t-suzuki@pha.nihon-u.ac.jp
Biological & pharmaceutical bulletin.Biol Pharm Bull.2002 Oct;25(10):1351-5.
The influx transport mechanism of pentazocine (PTZ) at the blood-brain barrier (BBB) was investigated in rats using the carotid injection technique. The uptake kinetics of PTZ into the rat brain exhibited saturability, which occurred by both nonsaturable and carrier-mediated transport processes. The
PMID 12392093

Japanese Journal

拮抗性鎮痛薬エプタゾシンによる術後硬膜外持続投与の有用性

今久子,山蔭道明,古瀬晋吾,永井荘一郎,並木昭義
日本臨床麻酔学会誌 = The Journal of Japan Society for Clinical Anesthesia 26(5), 594-601, 2006-09-15
NAID 10018309185

Postoperative Pain Relief by Epidural Infusion of Opioids in Patients Undergoing Haemorrhoidectomy

東博,辻仲康伸
日本大腸肛門病学会雑誌 58(2), 112-117, 2005
… 2 days) epidural administration of bupivacaine group (CB, n=22), continuous bupivacaine-morphine mixed group (CBM, n=22), continuous morphine (CM, n=21), continuous buprenorphine (CBP, n=18), continuous eptazocine group (CE, n=14) and diclofenac suppository group as a control group (CO, n=30). …
NAID 130000787608

Investigation on the Influx Transport Mechanism of Pentazocine at the Blood-Brain Barrier in Rats Using the Carotid Injection Technique(Biopharmacy)

Suzuki Toyofumi,Moriki Yoshiaki,Goto Hiroko [他],TOMONO Kazuo,HANANO Manabu,WATANABE Jun
Biological & pharmaceutical bulletin 25(10), 1351-1355, 2002-10-01
… In addition, narcotic-antagonist analgesic (buprenorphine, butorphanol or eptazocine) and an opioid antagonist (naloxone) significantly inhibited PTZ transport. …
NAID 110003638909

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★リンクテーブル★

リンク元	「エプタゾシン」
拡張検索	「eptazocine hydrobromide」

「エプタゾシン」

Eptazocine
Systematic (IUPAC) name
	(1S,6S)-1,4-dimethyl-2,3,4,5,6,7-hexahydro-1H-1,6-methano-4-benzazonin-10-ol
Clinical data
Pregnancy cat.	?
Legal status	℞ Prescription only
Routes	Oral
Identifiers
CAS number	72522-13-5; 72150-17-5 (bromide)
ATC code	None
PubChem	CID 3042090
ChemSpider	2305268
UNII	2208ZLI77S
Chemical data
Formula	C15H21NO
Mol. mass	231.333 g/mol
	SMILES Oc1ccc2c(c1)[C@@]3(CCN(C[C@H](C2)C3)C)C;
	InChI InChI=1S/C15H21NO/c1-15-5-6-16(2)10-11(9-15)7-12-3-4-13(17)8-14(12)15/h3-4,8,11,17H,5-7,9-10H2,1-2H3/t11-,15-/m1/s1; Key:ZOWQTJXNFTWSCS-IAQYHMDHSA-N ;