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SML2331

Sigma-Aldrich

Perospirone hydrochloride

≥98% (HPLC)

동의어(들):

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

실험식(Hill 표기법):
C23H30N4O2S · HCl
CAS Number:
129273-38-7
Molecular Weight:
463.04
MDL number:
MFCD07771999
UNSPSC 코드:
12352200
NACRES:
NA.77

분석

≥98% (HPLC)

형태

powder

저장 조건

desiccated

색상

white to beige

solubility

DMSO: 2 mg/mL, clear

저장 온도

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

생화학적/생리학적 작용

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.

픽토그램

Exclamation mark
GHS07

신호어

Warning

유해 및 위험 성명서

H302

예방조치 성명서

P264 - P270 - P301 + P312 - P501

Hazard Classifications

Acute Tox. 4 Oral

Storage Class Code

11 - Combustible Solids

WGK

WGK 1

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable

시험 성적서(COA)

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문서 라이브러리 방문

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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