Mesoridazine besylate
Modify Date: 2024-01-04 14:05:33
Mesoridazine besylate structure
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Common Name | Mesoridazine besylate | ||
|---|---|---|---|---|
| CAS Number | 32672-69-8 | Molecular Weight | 544.74900 | |
| Density | N/A | Boiling Point | 570.5ºC at 760mmHg | |
| Molecular Formula | C27H32N2O4S3 | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | 298.9ºC | |
| Symbol |
GHS07 |
Signal Word | Warning | |
Use of Mesoridazine besylateMesoridazine (TPS-23) benzenesulfonate, a metabolite of Thioridazine (HY-B0965A), acts as an orally active phenothiazine antipsychotic agent. Mesoridazine benzenesulfonate is a potent and rapid open-channel blocker of human ether-a-go-go related gene (hERG) channels and blocks hERG currents with an IC50 of 550 nM (at 0 mV) in human embryonic kidney 293 cells[1].Mesoridazine benzenesulfonate can be used for the research of schizophrenia, as well as certain other psychiatric disorders[1][2]. |
| Name | mesoridazine besylate |
|---|---|
| Synonym | More Synonyms |
| Description | Mesoridazine (TPS-23) benzenesulfonate, a metabolite of Thioridazine (HY-B0965A), acts as an orally active phenothiazine antipsychotic agent. Mesoridazine benzenesulfonate is a potent and rapid open-channel blocker of human ether-a-go-go related gene (hERG) channels and blocks hERG currents with an IC50 of 550 nM (at 0 mV) in human embryonic kidney 293 cells[1].Mesoridazine benzenesulfonate can be used for the research of schizophrenia, as well as certain other psychiatric disorders[1][2]. |
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| Related Catalog | |
| In Vitro | Mesoridazine blocks human ether-a-go-go-related gene (HERG) currents in a concentration-dependent manner (IC50 = 550 nM at 0 mV), block increased significantly over the voltage range where HERG activates and saturates at voltages eliciting maximal HERG channel activation[1]. Mesoridazine (15 mM; 24 h) shows total absorption of 15.94 ± 4.04% and 39.24 ± 5.11% in nude mouse and pig skin, respectively[3]. |
| In Vivo | Mesoridazine (15 mM; topical administration; once or daily for 7 consecutive days) displays potent activity and a long period of analgesia at blocking cutaneous pain[3]. Mesoridazine (15 mM) shows intradermal concentration of 0.34 0.74 nmol/mg after topical application on nude mouse back for 6 h[3]. Animal Model: Eight-week-old female nude mice[3] Dosage: 15 mM Administration: Topical administration, once (analgesia test) or daily for 7 consecutive days (irritation test) Result: Showed analgesic effect. A slight transepidermal water loss (TEWL) increased from 7.8 to 9.9 g/m2/h was observed. |
| References |
| Boiling Point | 570.5ºC at 760mmHg |
|---|---|
| Molecular Formula | C27H32N2O4S3 |
| Molecular Weight | 544.74900 |
| Flash Point | 298.9ºC |
| Exact Mass | 544.15200 |
| PSA | 130.81000 |
| LogP | 7.78380 |
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATAACUTE TOXICITY DATA
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| Symbol |
GHS07 |
|---|---|
| Signal Word | Warning |
| Hazard Statements | H302 |
| Precautionary Statements | P301 + P312 + P330 |
| Personal Protective Equipment | dust mask type N95 (US);Eyeshields;Gloves |
| Hazard Codes | Xn: Harmful; |
| Risk Phrases | 22 |
| RIDADR | NONH for all modes of transport |
| RTECS | DB7176700 |
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Thioridazine steady-state plasma concentrations are influenced by tobacco smoking and CYP2D6, but not by the CYP2C9 genotype.
Eur. J. Clin. Pharmacol. 59 , 45-50, (2003) Approximately 7% of Caucasians have genetically impaired activity of the cytochrome P450 enzyme CYP2D6 and are classified as poor metabolizers (PM). The disposition of thioridazine has been related to... |
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Inverse agonist actions of typical and atypical antipsychotic drugs at the human 5-hydroxytryptamine(2C) receptor.
J. Pharmacol. Exp. Ther. 299 , 83-89, (2001) Atypical antipsychotic drugs, which are distinguished from typical antipsychotic drugs by a lower incidence of extra-pyramidal side effects and less propensity to elevate serum prolactin levels (e.g.,... |
| benzenesulfonic acid,10-[2-(1-methylpiperidin-2-yl)ethyl]-2-methylsulfinylphenothiazine |
| 10-[2-(1-Methyl-2-piperidinyl)ethyl]-2-(methylsulfinyl)-10H-phenothiazine |
| Mesoridazine benzenesulfonate |