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Merck

SML2331

Sigma-Aldrich

Perospirone hydrochloride

≥98% (HPLC)

別名:

N-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]-1,2-cis-cyclohexanedicarboximide hydrochloride, SM-9018 hydrochloride, rel-(3aR,7aS)-2-[4-[4-(1,2-Benzisothiazol-3-yl)-1-piperazinyl]butyl]hexahydro-1H-isoindole-1,3(2H)-dione hydrochloride

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About This Item

実験式(ヒル表記法):
C23H30N4O2S · HCl
CAS番号:
分子量:
463.04
MDL番号:
UNSPSCコード:
12352200
NACRES:
NA.77

アッセイ

≥98% (HPLC)

形状

powder

保管条件

desiccated

white to beige

溶解性

DMSO: 2 mg/mL, clear

保管温度

2-8°C

InChI

1S/C23H30N4O2S.ClH/c28-22-17-7-1-2-8-18(17)23(29)27(22)12-6-5-11-25-13-15-26(16-14-25)21-19-9-3-4-10-20(19)30-24-21;/h3-4,9-10,17-18H,1-2,5-8,11-16H2;1H/t17-,18+;

InChI Key

HIZFAPMOZFYELI-GNXQHMNLSA-N

生物化学的/生理学的作用

Perospirone (SM-9018) is a typical neuroleptic (antipsychotic) agent that displays high affinity for 5-HT2, D2 and 5-HT1A receptors (Ki = 0.61, 1.4 and 2.9-1.8 nM, respectively), moderate affinity for alpha 1 and D1 receptors (Ki = 17 and 41 nM, respectively), while exhibiting much reduced affinity for alpha 2 (Ki = 408 nM) and little affinity toward muscarinic, opiate, glutamate, phencyclidine, benzodiazepine or GABAA receptors (Ki >1 μM). SM-9018 antagonizes both D2-dependent (e.g. methamphetamine-induced hyperactivity, apomorphine-induced stereotypy) and 5-HT2-mediated (e.g. tryptamine-induced clonic seizure) activities in vivo, while exhibiting very low cataleptogenic and central depressant activities commonly observed with two other neuroleptics, haloperidol and chlorpromazine.

ピクトグラム

Exclamation mark

シグナルワード

Warning

危険有害性情報

危険有害性の分類

Acute Tox. 4 Oral

保管分類コード

11 - Combustible Solids

WGK

WGK 1

引火点(°F)

Not applicable

引火点(℃)

Not applicable


適用法令

試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。

Jan Code

SML2331-VAR:
SML2331-5MG:
SML2331-BULK:
SML2331-25MG:


試験成績書(COA)

製品のロット番号・バッチ番号を入力して、試験成績書(COA) を検索できます。ロット番号・バッチ番号は、製品ラベルに「Lot」または「Batch」に続いて記載されています。

以前この製品を購入いただいたことがある場合

文書ライブラリで、最近購入した製品の文書を検索できます。

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T Kato et al.
Japanese journal of pharmacology, 54(4), 478-481 (1990-12-01)
The present study employed various receptor-binding assays to clarify the biochemical characteristics of SM-9018. SM-9018 possessed very high affinity for 5-HT2, D2 and 5-HT1A receptors (Ki = 0.61, 1.4 and 2.9 nM, respectively), and it had moderate affinity for alpha
Y Ohno et al.
Progress in neuro-psychopharmacology & biological psychiatry, 19(6), 1091-1101 (1995-10-01)
1. Receptor binding and behavioral studies were performed to compare the effects of subchronic treatments with SM-9018, a novel 5-HT2 and D2 antagonist, and with haloperidol (HAL) on dopamine and 5-HT receptors in rats. 2. SM-9018 treatment (10 mg/kg/day p.o.)
Kayoko Kanamitsu et al.
Drug metabolism and pharmacokinetics, 31(6), 395-404 (2016-10-18)
The effect of drugs in the central nervous system (CNS) is closely related to occupancy of their target receptor. In this study, we integrated plasma concentrations, in vitro/in vivo data for receptor or protein binding, and in silico data, using a physiologically
Y Ohno et al.
Pharmacology, biochemistry, and behavior, 49(1), 19-23 (1994-09-01)
Induction of bradykinesia by SM-9018, a novel 5-HT2 and D2 antagonist, was compared with that of other neuroleptics using the pole test in mice. Neuroleptics including SM-9018, haloperidol, chlorpromazine, and thioridazine dose dependently induced bradykinesia in the pole-descending behavior of
Y Maruoka et al.
Japanese journal of pharmacology, 62(4), 419-422 (1993-08-01)
The effects of SM-9018, a potential atypical neuroleptic, on monoamine metabolism were studied in rats. SM-9018 dose-dependently increased the levels of 3,4-dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA) in the cerebral cortex and striatum without affecting the levels of 5-HT

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