60-87-7 Usage
Description
As a derivative of phenothiazine, promethazine is structurally and pharmacologically similar
to chlorpromazine. It exhibits strong antihistamine activity as well as expressed action
on the CNS. It potentiates action of sedative and analgesic drugs.
Uses
Different sources of media describe the Uses of 60-87-7 differently. You can refer to the following data:
1. Promethazine is used for treating allergic illnesses such as hives, serum disease, hay
fever, dermatosis, and also for rheumatism with expressed allergic components, for allergic
complications caused by antibiotics and other medicinal drugs, and for enhancing
action of analgesics and local anesthetics. Synonyms of this drug are allergen, phenergan,
pipolphen, prothazine, and others.
2. Promethazine is used in preparation of antibodies having inhibitory activities to IL-36R signaling triggered by agonistic ligands and application to prevention and therapies of cancers and autoimmune diseases.
3. Anti-emetic; antihistaminic.
Definition
ChEBI: A tertiary amine that is a substituted phenothiazine in which the ring nitrogen at position 10 is attached to C-3 of an N,N-dimethylpropan-2-amine moiety.
World Health Organization (WHO)
Introduced in 1946, promethazine, a phenothiazine derivative has
a variety of pharmacological properties. At present it is mainly used as an
antihistamine and anti-motion-sickness drug. Promethazine is listed in the WHO
Model List of Essential Drugs.
General Description
Crystals. Melting point 60°C. Used as an antihistaminic.
Air & Water Reactions
Turns blue on prolonged exposure to air and moisture.
Reactivity Profile
PROMETHAZINE neutralizes acids in exothermic reactions to form salts plus water. May be incompatible with isocyanates, halogenated organics, peroxides, phenols (acidic), epoxides, anhydrides, and acid halides. Flammable or toxic gases may be generated in combination with strong reducing agents, such as hydrides.
Health Hazard
SYMPTOMS: Symptoms of PROMETHAZINE include leucopenia; agranulocytosis; confusion; convulsions; stupor; and it potentiates the action of central nervous system depressants.
Fire Hazard
Flash point data for PROMETHAZINE are not available, however PROMETHAZINE is probably combustible.
Clinical Use
Promethazine, an early agent in the series, has many useful pharmacological affects other
than being an antihistamine. It has significant antiemetic and anticholinergic properties. It
also has sedative-hypnotic properties and has been used to potentiate the effects of
analgesic drugs. Subsequent analogues, such as trimeprazine and methdilazine, are used as
antipruritic agents in the treatment of urticaria.
Safety Profile
Poison by ingestion,
intravenous, intramuscular, intraperitoneal,
and subcutaneous routes. Human systemic
effects by ingestion: pupillary dilation,
wakefulness, hallucinations, and distorted
perceptions. An experimental teratogen.
Other experimental reproductive effectsHuman mutation data reported. A severe
eye irritant. When heated to decomposition
it emits very toxic fumes of NOx and SOx
Synthesis
Promethazine, 10-(2-dimethylaminopropyl)phenothiazine (16.1.18), is
synthesized by alkylating phenothiazine with 1-dimethylamino-2-propylchloride.
Check Digit Verification of cas no
The CAS Registry Mumber 60-87-7 includes 5 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 2 digits, 6 and 0 respectively; the second part has 2 digits, 8 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 60-87:
(4*6)+(3*0)+(2*8)+(1*7)=47
47 % 10 = 7
So 60-87-7 is a valid CAS Registry Number.
InChI:InChI=1/C17H20N2S/c1-13(18(2)3)12-19-14-8-4-6-10-16(14)20-17-11-7-5-9-15(17)19/h4-11,13H,12H2,1-3H3
60-87-7Relevant articles and documents
Side-Chain Effects on Phenothiazine Cation Radical Reactions
Sackett, Patricia Holt,Mayausky, J. S.,Smith, Theresa,Kalus, Susan,McCreery, Richard L.
, p. 1342 - 1347 (1981)
The cation radical of each of the phenothiazine tranquilizers is a likely intermediate in the metabolism of the drugs to at least two of the three major metabolic classes, the sulfoxides and the hydroxylated derivatives.Previous work has shown that the reactions of the radical are highly dependent on the environment, patricularly the presence of nucleophiles.The present report discusses the effect of cation radical structure on the formation of sulfoxide and hydroxylated metabolites in vitro.Cyclic voltammetry, spectrophotometry, and liquid chromatography were used to examine reactions of various phenothiazine radicals in aqueous buffers.A radical with a three-carbon aliphatic side chain (e.g., chlorpromazine) forms solely sulfoxide and parent unless amine nucleophiles are present, in which case hydroxylation occurs.A shorter side chain (e.g., promethazine) causes radical dimerization and pronounced hydroxylation, regardless of external nucleophiles.A piperazine side chain (e.g., fluphenazine) promotes hydroxylation, with some sulfoxide observed.The results indicate that a deprotonated amine is necessary for hydroxylation and that the amine may be present in the original drug rather than an external nucleophile.In addition to information about cation radical reactions, the redox properties of several different phenothiazines are presented.
AMYLOID-BINDING COMPOUNDS AND METHODS OF USE THEREOF
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Paragraph 0078-0079, (2021/01/25)
A method of screening for amyloid-binding compounds, amyloid-binding compounds, and a method of detecting amyloid-β (Abeta) plaques in a subject are disclosed. The method of screening for amyloid-binding compounds includes combining amyloid, a dye, and at least one test compound to form a sample solution; equilibrating the sample solution; measuring a fluorescence signal of the sample solution; and comparing the measured fluorescence signal of the sample to a control; wherein attenuation of the fluorescence signal, as compared to the control, indicates that one or more of the test compounds bind amyloid. The amyloid-binding compound includes a compound detected by the screening method. The method of detecting amyloid-β (Abeta) plaques in a subject includes administering one or more of the amyloid-binding compounds to the subject, and detecting the compound within the subject.
Coupling body-benzonorbornene oligomer- (by machine translation)
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Paragraph 0189, (2016/10/07)
The invention relates to (among other things) oligomer-phenothiazine conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over un-conjugated phenothiazine compounds.
