Chlormezanone   中文名称: 氯美扎酮

使用抑制对侧伸肌超过 80% 的氯美扎宗剂量获得的比较结果 [1]。

Absorption, Distribution and Excretion
RAPIDLY ABSORBED FROM GI TRACT...EFFECT WITHIN 15 TO 30 MIN...DURATION OF ACTION OF 4 TO 6 HR...FREE DRUG & /4-CHLOROHIPPURIC ACID/ EXCRETED IN URINE /HUMAN, ORAL/...PRESENT IN HIGH CONCN IN KIDNEY, LIVER, MUSCLE, HEART, & BODY FAT, & IN LESSER CONCN IN LUNG & PLASMA /RATS, ORAL/.
AFTER ORAL ADMIN OF (14)C-CHLORMEZANONE, ABOUT 74% OF DOSE WAS EXCRETED INTO URINE OF RATS WITHIN 24 HR & 21% INTO URINE OF MICE WITHIN 2 HR. BILIARY EXCRETION OF RADIOACTIVITY WAS ABOUT 10% OF DOSE IN RATS.

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Metabolism / Metabolites
CHLORMEZANONE...IS EXCRETED UNCHANGED IN HUMAN URINE & DOG BILE. FORMATION OF 4-CHLOROHIPPURIC ACID, MAJOR URINARY METABOLITE IN MAN, INVOLVES NON-ENZYMIC HYDROLYSIS, FOLLOWED BY OXIDATION & CONJUGATION OF 4-CHLOROBENZALDEHYDE PRODUCT OF HYDROLYSIS.
(14)C-CHLORMEZANONE, METABOLITES IN URINE OF RATS & MICE WERE P-CHLOROBENZOIC ACID, P-CHLOROHIPPURIC ACID, N-METHYL-P-CHLOROBENZAMIDE, 2-[N-METHYL-N-(P-CHLOROBENZOYL)]CARBAMOYLETHYLSULFONIC ACID, 3-SULFOPROPIONIC ACID & GLUCURONIDE OF P-CHLOROBENZOIC ACID.

Toxicity Summary
Chlormezanone binds to central benzodiazepine receptors which interact allosterically with GABA receptors. This potentiates the effects of the inhibitory neurotransmitter GABA, increasing the inhibition of the ascending reticular activating system and blocking the cortical and limbic arousal that occurs following stimulation of the reticular pathways.

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Interactions
CHLORMEZANONE MAY LOWER TOLERANCE OF PATIENTS TO ALCOHOL...POSSIBLE ADDITIVE EFFECTS /WITH CHLORMEZANONE &/ CNS DEPRESSANTS SUCH AS ALCOHOL, PHENOTHIAZINES, BARBITURATES, NARCOTICS, OTHER PSYCHOTHERAPEUTIC AGENTS, & MONOAMINE OXIDASE INHIBITORS.

[1]. EFFECTS OF NEW s-TRIAZOLOBENZODIAZEPINE (D-4OTA) AND OTHER CENTRAL MUSCLE RELAXANTS ON SPINAL AND SUPRASPINAL REFLEXES IN CATS. Japan. J. Pharmacol, 23, 83-96 (1973).

Chlormezanone is a 1,3-thiazine that is 1,3-thiazinan-4-one S,S-dioxide in which a hydrogen at position 2 is substituted by a 4-chlorophenyl group and the hydrogen attached to the nitrogen is substituted by methyl. A non-benzodiazepine muscle relaxant, it was used in the management of anxiety and in the treatment of muscle spasms until being discontinued worldwide by its manufacturer in 1996, due to rare but serious cutaneous reactions. It has a role as an anxiolytic drug, a muscle relaxant and an antipsychotic agent. It is a 1,3-thiazine, a lactam, a sulfone and a member of monochlorobenzenes.
A non-benzodiazepine that is used in the management of anxiety. It has been suggested for use in the treatment of muscle spasm.
Chlormezanone is only found in individuals that have used or taken this drug. It is a non-benzodiazepine that is used in the management of anxiety. It has been suggested for use in the treatment of muscle spasm. [PubChem]Chlormezanone binds to central benzodiazepine receptors which interact allosterically with GABA receptors. This potentiates the effects of the inhibitory neurotransmitter GABA, increasing the inhibition of the ascending reticular activating system and blocking the cortical and limbic arousal that occurs following stimulation of the reticular pathways.
A non-benzodiazepine that is used in the management of anxiety. It has been suggested for use in the treatment of muscle spasm.

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Drug Indication
Used in the management of anxiety and in the treatment of muscle spasm.

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Mechanism of Action
Chlormezanone binds to central benzodiazepine receptors which interact allosterically with GABA receptors. This potentiates the effects of the inhibitory neurotransmitter GABA, increasing the inhibition of the ascending reticular activating system and blocking the cortical and limbic arousal that occurs following stimulation of the reticular pathways.
NEURONAL CONDUCTION, NEUROMUSCULAR TRANSMISSION, & MUSCLE EXCITABILITY ARE NOT DEPRESSED EXCEPT AFTER NEARLY LETHAL DOSES. PROMINENT EFFECT...IS TO DEPRESS SPINAL POLYSYNAPTIC REFLEXES PREFERENTIALLY OVER MONOSYNAPTIC REFLEXES. /CENTRALLY ACTING MUSCLE RELAXANTS/
IN ABSENCE OF DEFINITIVE STUDIES IT APPEARS REASONABLE TO ASCRIBE BENEFICIAL EFFECTS...TO THEIR SEDATIVE PROPERTIES. /CENTRALLY ACTING MUSCLE RELAXANTS/

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Therapeutic Uses
Anti-Anxiety Agents; Muscle Relaxants, Central
...ADMIN IV HAVE ESTABLISHED VALUE IN TREATING ACUTE MUSCLE SPASMS ASSOC WITH TRAUMA & INFLAMMATION. ...ALSO BENEFICIAL IN PRODUCING MUSCLE RELAXATION FOR CERTAIN ORTHOPEDIC MANIPULATIONS. ...MAY TEMPORARILY ABATE SOME OF SYMPTOMS OF CEREBRAL PALSY... /CENTRALLY ACTING MUSCLE RELAXANTS/
MANY AGENTS WITH MUSCLE RELAXANT PROPERTIES PRODUCE NOTABLE SEDATION IN ORDINARY ORAL DOSES. SUCH AGENTS ENJOY PARTICULARLY WIDE USE IN TREATMENT OF MUSCLE TENSION & PAINS ASSOC WITH ANXIETY STATES & PSYCHOSOMATIC DISORDERS. /CENTRALLY ACTING MUSCLE RELAXANTS/
MUSCLE RELAXANTS CAUSE SKELETAL MUSCULAR RELAXATION, WITHOUT LOSS OF CONSCIOUSNESS, AS RESULT OF SELECTIVE ACTION UPON CNS. ... ALL TYPES OF EXPTL HYPERTONIA & HYPERREFLEXIA...PRODUCED BY SPINAL OR SUPRASPINAL LESIONS, ARE DIMINISHED... ALSO...PROTECTION AGAINST...CONVULSIVE AGENTS... /CENTRALLY ACTING MUSCLE RELAXANTS/
...AS EFFECTIVE AS CHLORDIAZEPOXIDE IN TREATING MILD ANXIETY. MUSCULOSKELETAL DISORDERS IN WHICH ANXIETY & TENSION INTENSIFY SYMPTOMS MAY RESPOND TO ITS SEDATIVE EFFECT...DOES NOT APPEAR TO HAVE ANY SPECIFIC EFFECT ON SPASTICITY OR RIGIDITY ASSOC WITH ORG NEUROLOGIC DISORDERS.

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Drug Warnings
SOMETIMES METABOLITE DISCOLORS URINE.
UNTOWARD EFFECTS ARE GENERALLY MILD & OCCUR RELATIVELY INFREQUENTLY BUT, IN 2 CONTROLLED STUDIES, REACTIONS WERE MORE COMMON...THAN WITH CHLORDIAZEPOXIDE.
...PRODUCE SOME SEDATION, @ LEAST @ HIGHEST DOSES EMPLOYED CLINICALLY. /CENTRALLY ACTING MUSCLE RELAXANTS/

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Pharmacodynamics
Chlormezanone is a non-benzodiazepine muscle relaxant. It was discontinued worldwide in 1996 by its manufacturer due to confirmed serious and rare cutaneous reactions (toxic epidermal necrolysis).

C11H12CLNO3S

273.74

273.022

80-77-3

2717

White to off-white solid powder

1.4±0.1 g/cm3

534.5±50.0 °C at 760 mmHg

114ºC

277.1±30.1 °C

0.0±1.4 mmHg at 25°C

1.580

0.86

62.83

0

3

1

17

395

0

WEQAYVWKMWHEJO-UHFFFAOYSA-N

InChI=1S/C11H12ClNO3S/c1-13-10(14)6-7-17(15,16)11(13)8-2-4-9(12)5-3-8/h2-5,11H,6-7H2,1H3

2-(4-chlorophenyl)-3-methyl-1,1-dioxo-1,3-thiazinan-4-one

Trancopal; Chlormethazanone; Chlormezanone

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ≥ 100 mg/mL (~365.31 mM)
H2O : ~0.67 mg/mL (~2.45 mM)

配方 1 中的溶解度: ≥ 3.25 mg/mL (11.87 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 32.5 mg/mL澄清DMSO储备液加入到400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 3.25 mg/mL (11.87 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 32.5 mg/mL 澄清 DMSO 储备液加入 900 μL 20% SBE-β-CD 生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 3 中的溶解度: ≥ 3.25 mg/mL (11.87 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 32.5 mg/mL 澄清 DMSO 储备液加入900 μL 玉米油中，混合均匀。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。