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メトジラジン·塩酸塩

Methdilazine Hydrochloride

HCID 14676
ノート反応
基本情報概要名称と識別子物性安全と法規制化学と産業関連反応化合物ノート
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基本情報

CAS
1229-35-2
標準SMILES
CN1CCC(CN2c3ccccc3Sc3ccccc32)C1.Cl
InChIKey
IEISBKIVLDXSMZ-UHFFFAOYSA-N
分子式
C18H20N2S.ClH
平均分子量
332.9 g/mol
単同位体質量
332.1113975

概要

Methdilazine hydrochloride is a white microcrystalline powder with a slight odor. pH (1% aqueous solution) 4.8-6. (NTP, 1992)

名称と識別子

優先名称
Methdilazine Hydrochloride
IUPAC
10-[(1-methylpyrrolidin-3-yl)methyl]phenothiazine;hydrochloride
現地名
メトジラジン·塩酸塩
英語名
METHDILAZINE HYDROCHLORIDE (200 MG)
分子式
C18H21ClN2S
分子量
332.89074

名称と別名

METHDILAZINE HYDROCHLORIDE1229-35-2Methdilazine HclDisyncranTacaryl hydrochlorideMethdilazine monohydrochlorideDTXSID3025548MJ 5022T0GSO02UEZNSC-169091CHEBI:140855DTXCID905548
名称をさらに表示
メトジラジン·塩酸塩10-[(1-メチルピロリジン-3-イル)メチル]-10H-フェノチアジン·塩酸塩メトジラジン塩酸塩塩酸メトジラジンメトジラジン・塩酸塩10-[(1-メチルピロリジン-3-イル)メチル]-10H-フェノチアジン・塩酸塩dilosymBristalineMETHADILAZINEHCLmethdilazinehydrochlorideMethilazine hydrochlorideRanolazine Impurity 18-d5METHDILAZINE HYDROCHLORIDE (200 MG)
Methdilazine hydrochloride (USP)Methdilazine hydrochloride [USP]Phenothiazine, 10-((1-methyl-3-pyrrolidinyl)methyl)-, hydrochloridePhenothiazine, 10-((1-methyl-3-pyrrolidinyl)methyl)-, monohydrochloride10H-Phenothiazine, 10-((1-methyl-3-pyrrolidinyl)methyl)-, monohydrochloride10-[(1-Methyl-3-pyrrolidinyl)methyl]phenothiazine hydrochlorideDisyncram10-((1-methyl-3-pyrrolidinyl)methyl)phenothiazine hydrochloride

物性

構造計算による物性

極性表面積
31.8 Ų
水素結合供与体数
1
水素結合受容体数
3
回転可能結合数
2
重原子数
22
形式電荷
0
複雑度
339

実験および物理化学的性質

pHBETWEEN 4.8 AND 6.0 (1 IN 100 SOLN)
OdorSLIGHT, CHARACTERISTIC
TasteBITTER, ANESTHETIC
Color/Form · 2 件

LIGHT-TAN, CRYSTALLINE POWDER

CRYSTALS FROM ISOPROPYL ALCOHOL

Solubility · 2 件

50 to 100 mg/mL at 63 °F (NTP, 1992)

1 G IN 2 ML WATER, 2 ML ALC, 6 ML CHLOROFORM, MORE THAN 10,000 ML ETHER

Human Drugs · 2 件

FDA approved drugs -> Active ingredient

FDA approved drugs -> Active ingredient

Melting Point · 2 件

370 to 372 °F (NTP, 1992)

187.5-189 °C

Physical DescriptionMethdilazine hydrochloride is a white microcrystalline powder with a slight odor. pH (1% aqueous solution) 4.8-6. (NTP, 1992)

物理化学的性質

融点
187.5 · 187.5-189°
貯蔵温度
Sealed in dry,Room Temperature

安全と法規制

安全情報は参考情報です。供給元の安全データシート(SDS)、適用法令、専門家による評価に代わるものではありません。

危険有害性情報

Regulatory Information10H-Phenothiazine, 10-(1-methyl-3-pyrrolidinyl)methyl-, monohydrochloride: Does not have an individual approval but may be used under an appropriate group standard
Fire HazardsFlash point data for this chemical are not available; however, it is probably combustible. (NTP, 1992)
Health Hazards · 1 件

SYMPTOMS: Symptoms of exposure to this compound may include drowsiness, dizziness, lassitude, tinnitus, incoordination, fatigue, blurred vision, euphoria, diplopia, nervousness, insomnia, tremors, grand mal seizures, catatonic-like states, neuritis and hysteria. It may cause bradycardia, cardiac arrest, anorexia, epigastric distress, constipation, dry mouth, urticaria, dermatitis, asthma, laryngeal edema, photosensitivity, lupus erythematous-like syndrome, anaphylactoid reactions, leukopenia, agranulocytosis, thrombocytopenic purpura and jaundice of the obstructive type. In children, symptoms may include excitation, hallucinations, convulsions and sudden death. In elderly people, it may cause hypotension, syncope, toxic confusional states, excessive sedation, extrapyramidal signs, akathisia and persistent dyskinesia.

FDA Requirements · 1 件

Manufacturers, packers, and distributors of drug and drug products for human use are responsible for complying with the labeling, certification, and usage requirements as prescribed by the Federal Food, Drug, and Cosmetic Act, as amended (secs 201-902, 52 Stat. 1040 et seq., as amended; 21 U.S.C. 321-392).

Reactive GroupAmines, Phosphines, and Pyridines
Reactivity Profile · 1 件

METHDILAZINE HYDROCHLORIDE is sensitive to exposure to light. (NTP, 1992) An acidic salt. Materials in this group are generally soluble in water. The resulting solutions contain moderate concentrations of hydrogen ions and have pH's of less than 7.0. They react as acids to neutralize bases. These neutralizations generate heat, but less or far less than is generated by neutralization of inorganic acids, inorganic oxoacids, and carboxylic acid. They usually do not react as either oxidizing agents or reducing agents but such behavior is not impossible.

化学と産業

薬理情報

Mechanism of Action · 5 件

Antihistamines used in the treatment of allergy act by competing with histamine for H1-receptor sites on effector cells. They thereby prevent, but do not reverse, responses mediated by histamine alone. Antihistamines antagonize, in varying degrees, most of the pharmacological effects of histamine, including urticaria and pruritus. In addition, the anticholinergic actions of most antihistamines provide a drying effect on the nasal and oral mucosa. /Antihistamines, phenothiazine-derivative/

H1 antagonists inhibit most responses of smooth muscle to histamine. Antagonism of the constrictor action of histamine on respiratory smooth muscle is easily shown in vivo and in vitro. /Histamine Antagonists: H1 Antagonists/

H1 antagonists strongly block the action of histamine that results in increased permeability and formation of edema and wheal. /Histamine Antagonists: H1 Antagonists/

Within the vascular tree, the H1 antagonists inhibit both the vasoconstrictor effects of histamine and, to a degree, the more rapid vasodilator effects that are mediated by H1 receptors on endothelial cells. Residual vasodilatation reflects the involvement of H2 receptors on smooth muscle and can be suppressed only by the concurrent administration of an H2 antagonist. Effects of the histamine antagonists on histamine-induced changes in systemic blood pressure parallel these vascular effects. /Histamine Antagonists: H1 Antagonists/

Many of the H1 antagonists tend to inhibit responses to acetylcholine that are mediated by muscarinic receptors. These atropine-like actions are sufficiently prominent in some of the drugs to be manifest during clinical usage ... . /Histamine Antagonists: H1 Antagonists/

Metabolism/Metabolites · 2 件

MAIN SITE OF METABOLIC TRANSFORMATION IS LIVER. /ANTIHISTAMINES/

H1 blockers are among the many drugs that induce hepatic microsomal enzymes, and they may facilitate their own metabolism. /Histamine Antagonists: H1 Antagonists/

Absorption, Distribution and Excretion · 3 件

Well absorbed after oral administration. /Antihistamines, phenothiazine-derivative/

The H1 antagonists are well absorbed from the GI tract. Following oral administration, peak plasma concn are achieved in 2 to 3 hr and effects usually last 4 to 6 hr; however, some of the drugs are much longer acting ... . /Histamine Antagonists: H1 Antagonists/

関連反応

0 件
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化合物ノート

読み込み中…

このページの内容基本情報概要名称と識別子物性安全と法規制化学と産業関連反応化合物ノート

データベース識別子

CAS
1229-35-2
PubChem CID
14676
DTXSID
DTXSID3025548
ChEMBL
CHEMBL1200532
ChEBI
CHEBI:140855
UNII
T0GSO02UEZ
EC Number
214-967-3
溶解性
DMSO (Slightly), Methanol (Slightly), Water (Slightly)
外見
Solid
色
Off-White to Pale Brown
安定性
Air Sensitive, Hygroscopic
EPAの化学物質情報
Methdilazine hydrochloride (1229-35-2)
Air and Water ReactionsWater soluble. pH (1% aqueous solution) 4.8-6 (NTP, 1992).

安全と保護具

Fire FightingFires involving this material can be controlled with a dry chemical, carbon dioxide or Halon extinguisher. (NTP, 1992)
First Aid · 1 件

EYES: First check the victim for contact lenses and remove if present. Flush victim's eyes with water or normal saline solution for 20 to 30 minutes while simultaneously calling a hospital or poison control center. Do not put any ointments, oils, or medication in the victim's eyes without specific instructions from a physician. If symptoms (such as redness or irritation) develop, immediately transport the victim to a hospital.

Nonfire Spill Response · 1 件

SMALL SPILLS AND LEAKAGE: If you spill this chemical, you should dampen the solid spill material with water, then transfer the dampened material to a suitable container. Use absorbent paper dampened with water to pick up any remaining material. Seal your contaminated clothing and the absorbent paper in a vapor-tight plastic bag for eventual disposal. Wash all contaminated surfaces with a soap and water solution. Do not reenter the contaminated area until the Safety Officer (or other responsible person) has verified that the area has been properly cleaned.

Disposal Methods · 1 件

SRP: At the time of review, criteria for land treatment or burial (sanitary landfill) disposal practices are subject to significant revision. Prior to implementing land disposal of waste residue (including waste sludge), consult with environmental regulatory agencies for guidance on acceptable disposal practices.

Personal Protective Equipment (PPE) · 1 件

RECOMMENDED RESPIRATOR: Where the neat test chemical is weighed and diluted, wear a NIOSH-approved half face respirator equipped with an organic vapor/acid gas cartridge (specific for organic vapors, HCl, acid gas and SO2) with a dust/mist filter. (NTP, 1992)

毒性情報

Interactions · 5 件

METHDILAZINE HYDROCHLORIDE (3 MG/KG IP) POTENTIATED THE PENTOBARBITONE INDUCED HYPNOSIS IN RATS.

Concurrent use /with alcohol or other CNS depression-producing medications/ may potentiate the CNS depressant effects of either these medications or antihistamines; also, concurrent use of maprotiline or tricyclic antidepressants may potentiate the anticholinergic effects of either antihistamines or these medications. /Antihistamines, phenothiazine-derivative/

Concurrent use /with amphetamines/ may decrease stimulant effects of amphetamines since phenothiazine derivatives produce alpha-adrenergic blockage. /Antihistamines, phenothiazine-derivative/

Anticholinergic effects may be potentiated when /anticholinergics or other medications with anticholinergic activity/ are used concurrently with antihistamines; patients should be advised to report occurrence of gastrointestinal problems promptly since paralytic ileus may occur with concurrent therapy. /Antihistamines, phenothiazine-derivative/

For more Interactions (Complete) data for METHDILAZINE HYDROCHLORIDE (21 total), please visit the HSDB record page.

Exposure RoutesWell absorbed in the digestive tract.
Toxicity SummaryMethdilazine binds to the histamine H<sub>1</sub> receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine.
Signs and Symptoms · 1 件

Symptoms of overdose include clumsiness or unsteadiness, convulsions, drowsiness, dryness of mouth, nose, or throat, feeling faint, flushing or redness of face, hallucinations, muscle spasms (especially of neck and back), restlessness, shortness of breath or troubled breathing, shuffling walk, tic-like movements of head and face, trembling and shaking of hands, and trouble in sleeping.

Ongoing Test Status · 1 件

The following link will take the user to the National Toxicology Program (NTP) Test Agent Search Results page, which tabulates all of the "Standard Toxicology & Carcinogenesis Studies", "Developmental Studies", and "Genetic Toxicity Studies" performed with this chemical. Clicking on the "Testing Status" link will take the user to the status (i.e., in review, in progress, in preparation, on test, completed, etc.) and results of all the studies that the NTP has done on this chemical. /Methdilazine/ [http://ntp-apps.niehs.nih.gov/ntp_tox/index.cfm?fuseaction=ntpsearch.searchresults&searchterm=1982-37-2]

Human Toxicity Excerpts · 5 件

ADVERSE EFFECTS INCLUDE DROWSINESS, DIZZINESS, GASTROINTESTINAL DISTURBANCES, DRYNESS OF THE MUCOUS MEMBRANES, HEADACHE AND SKIN RASH. EXTRAPYRAMIDAL SYMPTOMS HAVE ALSO BEEN REPORTED. OTHER UNTOWARD REACTIONS MAY INCLUDE THOSE FOR PHENOTHIAZINES IN GENERAL.

In acute poisoning with H1 antagonists, their central excitatory effects constitute the greatest danger. The syndrome includes hallucinations, excitement, ataxia, incoordination, athetosis, and convulsions. Fixed, dilated pupils with a flushed face, together with sinus tachycardia, urinary retention, dry mouth, and fever, lend the syndrome a remarkable similarity to that of atropine poisoning. Terminally, there is deepening coma with cardiorespiratory collapse and death, usuallY within 2 to 18 hours. Treatment is along general symptomatic and supportive lines. /Histamine Antagonists: H1 Antagonists/

... SIDE EFFECTS INCL DRYNESS OF ... RESP PASSAGES, SOMETIMES INDUCING COUGH; URINARY FREQUENCY & DYSURIA; PALPITATION; HYPOTENSION; HEADACHE; TIGHTNESS OF CHEST; TINGLING, HEAVINESS, & WEAKNESS OF HANDS. ... ALLERGIC DERMATITIS IS NOT UNCOMMON. /ANTIHISTAMINES/

IN SMALL CHILD ... SYNDROME OF POISONING INCL ... ATAXIA, INCOORDINATION, ATHETOSIS ... FIXED, DILATED PUPILS WITH FLUSHED FACE ... ARE COMMON. /ANTIHISTAMINES/

ALTHOUGH H1-BLOCKING DRUGS HAVE RELATIVELY HIGH MARGIN OF SAFETY, ACUTE POISONING WITH THEM IS COMMON. ... IN CHILDREN, 20 TO 30 TABLETS OR CAPSULES OF MOST COMMERCIALLY AVAILABLE ANTIHISTAMINES REPRESENTS LETHAL OR NEAR-LETHAL DOSE. /ANTIHISTAMINES/

Carcinogen ClassificationNo indication of carcinogenicity to humans (not listed by IARC).
Non-Human Toxicity ExcerptsSome H1 antagonists possess local anesthetic activity ... . /Histamine Antagonists: H1 Antagonists/
Populations at Special Risk · 2 件

Use is not recommended in newborn or premature infants because this age group has an increased susceptibility to anticholinergic side effects, such as central nervous system excitation, and an increased tendency toward convulsions. /Antihistamines, phenothiazine-derivative/

The use of phenothiazine-derivative antihistamines is not recommended in infants up to 3 months of age, because of the possible absence or deficiency of detoxifying enzyme and inefficient renal function usually noted in this age group. Also, increased susceptibility to dystonias has been reported in newborn or premature infants, acutely ill or dehydrated children, and children with acute infections who have received phenothiazine medication. /Antihistamines, phenothiazine-derivative/

Antidote and Emergency Treatment · 1 件

THERE IS NO SPECIFIC THERAPY FOR ANTIHISTAMINE POISONING, AND TREATMENT IS ALONG GENERAL SYMPTOMATIC AND SUPPORTIVE LINES. ... SHOULD BREATHING FAIL, MECH SUPPORT OF VENTILATION OFFER SAFER AND ... EFFECTIVE MEANS OF MAINTAINING RESP THAN USE OF ANALEPTICS WHICH ARE PRONE TO INITIATE OR INTENSIFY CONVULSIVE PHASE. /ANTIHISTAMINES/

法規制情報

FDA Requirements · 1 件

Manufacturers, packers, and distributors of drug and drug products for human use are responsible for complying with the labeling, certification, and usage requirements as prescribed by the Federal Food, Drug, and Cosmetic Act, as amended (secs 201-902, 52 Stat. 1040 et seq., as amended; 21 U.S.C. 321-392).

安全データ

ridadr
UN 2811 6.1 / PGIII
毒性
LD50 orally in rats: 320 mg/kg (Goldenthal)
hs_code
2934302700
有毒物質データの
1229-35-2(Hazardous Substances Data)

... H1 antagonists are eliminated more rapidly by children than by adults and more slowly in those with severe liver disease. /Histamine Antagonists: H1 Antagonists/

用途と製造

Uses · 2 件

MEDICATION

Used for the symptomatic relief of hypersensitivity reactions and particularly for the control of pruritic skin disorders

U.S. Production · 2 件

(1976) PROBABLY GREATER THAN 4.5X10+5 G /METHDILAZINE/

(1980) PROBABLY GREATER THAN 4.5X10+5 G /METHDILAZINE/

Consumption PatternsND /METHDILAZINE/
Methods of Manufacturing · 3 件

CONDENSATION OF DIMETHYL ITACONATE WITH METHYLAMINE, REDUCTION WITH LITHIUM ALUMINUM HYDRIDE & REACTION WITH THIONYL CHLORIDE TO FORM PHENOTHIAZINE, TNEN CONDENSATION WITH 1-METHYL-3-PYRROLIDINYLMETHYL CHLORIDE USING SODIUM OR LITHIUM AMIDE AS CONDENSING AGENT /METHDILAZINE/

METHDILAZINE IS REACTED WITH AN EQUIMOLAR QUANTITY OF HYDROGEN CHLORIDE IN A NONAQUEOUS SOLVENT.

FELDKAMP, WU, US PATENT 2,945,855 (1960 TO MEAD JOHNSON).

Formulations/PreparationsDibosyn, Disyncran, Tacaryl

応用分野

使用Antipruritic.

一般的な説明White microcrystalline powder with a slight odor. pH (1% aqueous solution) 4.8-6.

上流・下流製品情報

上流原料

塩酸フェノチアジン

サプライヤー17 社

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