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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/12/09 16:21:43」(JST)

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Mesoridazine (Serentil) is a piperidine neuroleptic drug belonging to the class of drugs called phenothiazines, used in the treatment of schizophrenia. It is a metabolite of thioridazine. The drug's name is derived from the methylsulfoxy and piperidine functional groups in its chemical structure.

It has central antiadrenergic, antidopaminergic, antiserotonergic and weak muscarinic anticholinergic effects.

Serious side effects include akathisia, tardive dyskinesia and the potentially fatal neuroleptic malignant syndrome.

Mesoridazine was withdrawn from the United States market in 2004 due to dangerous side effects, namely irregular heart beat and QT-prolongation of the electrocardiogram.^[1]

It currently appears to be unavailable worldwide.

References

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1. 第1世代抗精神病剤：薬理学、投与、および副作用の比較 first generation antipsychotic medications pharmacology administration and comparative side effects
2. 体重減少がみられる患者に対するアプローチ approach to the patient with weight loss
3. 精神病性特徴を伴う単極性大うつ病：急性期治療 unipolar major depression with psychotic features acute treatment
4. 第一世代（定型）抗精神病剤中毒 first generation typical antipsychotic medication poisoning
5. 抗コリン剤中毒 anticholinergic poisoning

English Journal

Oncologic outcomes of robotic-assisted total mesorectal excision for the treatment of rectal cancer.

Baek JH1, McKenzie S, Garcia-Aguilar J, Pigazzi A.Author information 1Department of Surgery, Gachon University of Medicine and Science, Gil Medical Center, Namdong-gu, Incheon, Korea.AbstractOBJECTIVE: To evaluate local recurrence and survival after robotic-assisted total mesorectal excision (RTME) for primary rectal cancer.
Annals of surgery.Ann Surg.2010 May;251(5):882-6. doi: 10.1097/SLA.0b013e3181c79114.
OBJECTIVE: To evaluate local recurrence and survival after robotic-assisted total mesorectal excision (RTME) for primary rectal cancer.SUMMARY BACKGROUND DATA: RTME is a novel approach for the treatment of rectal cancer and has been shown to be safe and effective. However, the oncologic results of t
PMID 20395863

Phenothiazine-type antipsychotics elicit cutaneous analgesia in rats.

Chen YW1, Chu CC, Chu KS, Shieh JP, Chien CC, Wang JJ, Kao CH.Author information 1Department of Medical Research, Chi Mei Medical Center, Tainan, Taiwan, R.O.C.AbstractBACKGROUND: Local anesthetics exert their anesthetic and analgesic effects by blocking the sodium channels in the nervous system. Phenothiazine-type antipsychotics also block sodium channels, but the local anesthetic characteristics of these drugs have not been evaluated. The aim of this study was to evaluate the cutaneous analgesic effect of phenothiazine-type antipsychotics.
Acta anaesthesiologica Taiwanica : official journal of the Taiwan Society of Anesthesiologists.Acta Anaesthesiol Taiwan.2010 Mar;48(1):3-7. doi: 10.1016/S1875-4597(10)60002-1.
BACKGROUND: Local anesthetics exert their anesthetic and analgesic effects by blocking the sodium channels in the nervous system. Phenothiazine-type antipsychotics also block sodium channels, but the local anesthetic characteristics of these drugs have not been evaluated. The aim of this study was t
PMID 20434106

Identification of novel substrates for human cytochrome P450 2J2.

Lee CA1, Neul D, Clouser-Roche A, Dalvie D, Wester MR, Jiang Y, Jones JP 3rd, Freiwald S, Zientek M, Totah RA.Author information 1Pfizer Global Research & Development, 10646 Science Center Dr., San Diego, CA 92121, USA. caroline.lee01@pfizer.comAbstractSeveral antihistamine drugs including terfenadine, ebastine, and astemizole have been identified as substrates for CYP2J2. The overall importance of this enzyme in drug metabolism has not been fully explored. In this study, 139 marketed therapeutic agents and compounds were screened as potential CYP2J2 substrates. Eight novel substrates were identified that vary in size and overall topology from relatively rigid structures (amiodarone) to larger complex structures (cyclosporine). The substrates displayed in vitro intrinsic clearance values ranging from 0.06 to 3.98 mul/min/pmol CYP2J2. Substrates identified for CYP2J2 are also metabolized by CYP3A4. Extracted ion chromatograms of metabolites observed for albendazole, amiodarone, astemizole, thioridazine, mesoridazine, and danazol showed marked differences in the regioselectivity of CYP2J2 and CYP3A4. CYP3A4 commonly metabolized compounds at multiple sites, whereas CYP2J2 metabolism was more restrictive and limited, in general, to a single site for large compounds. Although the CYP2J2 active site can accommodate large substrates, it may be more narrow than CYP3A4, limiting metabolism to moieties that can extend closer toward the active heme iron. For albendazole, CYP2J2 forms a unique metabolite compared with CYP3A4. Albendazole and amiodarone were evaluated in various in vitro systems including recombinant CYP2J2 and CYP3A4, pooled human liver microsomes (HLM), and human intestinal microsomes (HIM). The Michaelis-Menten-derived intrinsic clearance of N-desethyl amiodarone was 4.6 greater in HLM than in HIM and 17-fold greater in recombinant CYP3A4 than in recombinant CYP2J2. The resulting data suggest that CYP2J2 may be an unrecognized participant in first-pass metabolism, but its contribution is minor relative to that of CYP3A4.
Drug metabolism and disposition: the biological fate of chemicals.Drug Metab Dispos.2010 Feb;38(2):347-56. doi: 10.1124/dmd.109.030270. Epub 2009 Nov 18.
Several antihistamine drugs including terfenadine, ebastine, and astemizole have been identified as substrates for CYP2J2. The overall importance of this enzyme in drug metabolism has not been fully explored. In this study, 139 marketed therapeutic agents and compounds were screened as potential CYP
PMID 19923256

Japanese Journal

Mesoridazine(NC-123)の中枢作用補遺脳波および脊髄反射におよぼす影響

丸山昇治 [他]
新潟医学会雑誌 86(7), 330-338, 1972-07
NAID 40018191573

Mesoridazineの胎仔への影響試験

小嶋哲夫 [他]
新潟医学会雑誌 81(11), 625-630, 1967-11
NAID 40018191977

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リンク元

「メソリダジン」

Mesoridazine
Systematic (IUPAC) name
	10-{2-[(RS)1-Methylpiperidin-2-yl]ethyl}- 2-methylsulfinyl- 10H-phenothiazine
Clinical data
Trade names	Serentil
AHFS/Drugs.com	Micromedex Detailed Consumer Information
MedlinePlus	a682306
Pregnancy; category	US: C (Risk not ruled out); ;
Legal status	℞ (Prescription only);
Routes of; administration	oral, intravenous
Pharmacokinetic data
Protein binding	4%
Metabolism	Hepatic/Renal
Biological half-life	24 to 48 hours
Excretion	Biliary and renal
Identifiers
CAS Number	5588-33-0
ATC code	N05AC03
PubChem	CID: 4078
IUPHAR/BPS	7227
DrugBank	DB00933
ChemSpider	3936
UNII	5XE4NWM740
KEGG	D02671
ChEBI	CHEBI:6780
ChEMBL	CHEMBL1088
Chemical data
Formula	C21H26N2OS2
Molecular mass	386.576 g/mol
	SMILES O=S(c2cc1N(c3c(Sc1cc2)cccc3)CCC4N(C)CCCC4)C ;
	InChI InChI=1S/C21H26N2OS2/c1-22-13-6-5-7-16(22)12-14-23-18-8-3-4-9-20(18)25-21-11-10-17(26(2)24)15-19(21)23/h3-4,8-11,15-16H,5-7,12-14H2,1-2H3 ; Key:SLVMESMUVMCQIY-UHFFFAOYSA-N ;
Physical data
Melting point	130 °C (266 °F)
Solubility in water	insoluble mg/mL (20 °C)
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英: mesoridazine
化: ベシル酸メソリダジン mesoridazine besylate
商: Serentil
関: 抗精神病薬

統合失調症治療薬
フェノチアジン・ピペリジン系
おそらく日本では保険適応なし

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mesoridazine