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54-84-2

54-84-2 structure
54-84-2 structure
  • Name: Cinanserin hydrochloride
  • Chemical Name: cinanserin hydrochloride
  • CAS Number: 54-84-2
  • Molecular Formula: C20H25ClN2OS
  • Molecular Weight: 376.94300
  • Catalog: Signaling Pathways Anti-infection Influenza Virus
  • Create Date: 2017-12-27 18:08:32
  • Modify Date: 2025-08-25 11:22:56
  • Cinanserin hydrochloride (SQ 10643) is a potent, selective and highly affinity 5-HT2 receptor antagonist with a Ki of 41 nM. Cinanserin hydrochloride has a much higher binding affinity for the 5-HT2 than for the 5-HT1 receptor (Ki of 3500 nM). Cinanserin is also an inhibitor of 3C-like proteinase of severe acute respiratory syndrome coronavirus and strongly reduces virus replication in vitro[1][2][3].

Name cinanserin hydrochloride
Synonyms maptc
Cinnanserin
sq10,643
CINANSERIN
DPTC HYDROCHLORIDE
DPTC
Description Cinanserin hydrochloride (SQ 10643) is a potent, selective and highly affinity 5-HT2 receptor antagonist with a Ki of 41 nM. Cinanserin hydrochloride has a much higher binding affinity for the 5-HT2 than for the 5-HT1 receptor (Ki of 3500 nM). Cinanserin is also an inhibitor of 3C-like proteinase of severe acute respiratory syndrome coronavirus and strongly reduces virus replication in vitro[1][2][3].
Related Catalog
Target

Ki: 41 nM (5-HT2 receptor)[3]; 3C-like proteinase[1]

In Vitro Cinanserin/Cinanserin hydrochloride have binding affinity to SARS-CoV 3CLpro, HCoV-229E 3CLpro, with the KD values of 49.4 μM/78.0 μM for SARS-associated coronavirus (SARS-CoV) 3CLpro and 18.2 μM/36.6 μM for human coronavirus 229E (HCoV-229E) 3CLpro[1]. The IC50 values of Cinanserin and Cinanserin hydrochloride for inhibiting the catalytic activity of SARS-CoV 3CLpro are calculated as 4.92 μM and 5.05 μM, respectively, The corresponding IC50 values for HCoV-229E 3CLpro are 4.68 μM and 5.68 μM. None of the compounds have inhibitory activity against HRV-14 3Cpro at concentrations up to 200 μM[1].
In Vivo Cinanserin (5 mg/kg; intravenous injection; for 2 hours; male Wistar rats) treatment significantly reduces systemic burn edema to shamburn levels. Leukocyte-endothelial interactions are significantly reduced by administration of Cinanserin[2]. Animal Model: Male Wistar rats (250 g) underwent thermal injury[2] Dosage: 5 mg/kg Administration: Intravenous injection; for 2 hours Result: Significantly reduced systemic burn edema to shamburn levels..
References

[1]. Chen L, et al. Cinanserin is an inhibitor of the 3C-like proteinase of severe acute respiratory syndrome coronavirus and strongly reduces virus replication in vitro. J Virol. 2005 Jun;79(11):7095-103.

[2]. Hernekamp JF, et al. Cinanserin reduces plasma extravasation after burn plasma transfer in rats. Burns. 2013 Sep;39(6):1226-33.

[3]. Leysen JE, et al. Receptor binding profile of R 41 468, a novel antagonist at 5-HT2 receptors. Life Sci. 1981 Mar 2;28(9):1015-22.

Boiling Point 519.5ºC at 760mmHg
Molecular Formula C20H25ClN2OS
Molecular Weight 376.94300
Flash Point 268ºC
Exact Mass 376.13800
PSA 57.64000
LogP 5.25730

CHEMICAL IDENTIFICATION

RTECS NUMBER :
GD7478000
CHEMICAL NAME :
Cinnamanilide, 2'-((3-(dimethylamino)propyl)thio)-, monohydrochloride
CAS REGISTRY NUMBER :
54-84-2
LAST UPDATED :
199709
DATA ITEMS CITED :
4
MOLECULAR FORMULA :
C20-H24-N2-O-S.Cl-H
MOLECULAR WEIGHT :
376.98
WISWESSER LINE NOTATION :
1N1&3SR BMV1U1R &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
1500 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - changes in motor activity (specific assay)
REFERENCE :
AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 152,132,1964
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
480 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - changes in motor activity (specific assay)
REFERENCE :
AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 152,132,1964
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
35 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - changes in motor activity (specific assay)
REFERENCE :
AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 152,132,1964
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
8 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - changes in motor activity (specific assay)
REFERENCE :
AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 152,132,1964
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