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Dyclonine hydrochloride

Dyclonine hydrochloride structure

CAS No:
536-43-6
Formula:
C18H28ClNO2
Chemical Name:
Dyclonine hydrochloride
Synonyms:
DYCLONINE HCL;DYCLONINE HYDROCHLORIDE;LABOTEST-BB LT00771942;1-(4-BUTOXYPHENYL)-3-(1-PIPERIDINYL)-1-PROPANONE HCL;1-(4-BUTOXYPHENYL)-3-(1-PIPERIDINYL)-1-PROPANONE HYDROCHLORIDE;1-(4-butoxyphenyl)-3-(1-piperidinyl)-1-propanonhydrochloride;dyclonine hydrochlorideinoline-3-carboxylic acid;1-(4-butoxyphenyl)-3-(1-piperidinyl)-1-propanone chloride
Categories:
Active Pharmaceutical Ingredients > Anesthetic Agents

Description

Dyclonine is an oral anaesthetic found in Sucrets, an over the counter throat lozenge.Target: Sodium ChannelDyclonine is an oral anaesthetic that is the active ingredient of Sucrets, an over the counter throat lozenge. It is also found in some varieties of the Cepacol sore throat spray. It is a local anesthetic, used topically as the hydrochloride salt. Dyclonine hydrochloride has been found to possess, in addition to its topical anesthetic properties, significant bactericidal and fungic

Dyclonine Hydrochloride is the hydrochloride salt of Dyclonine, an unclassified compound with local anesthetic effect. Dyclonine reversibly binds to activated sodium channels on the neuronal membrane, thereby decreasing the neuronal membrane's permeability to sodium ions, leading to an increased threshold for excitation. This reversibly stabilizes the membrane and inhibits depolarization, leading to the failure of a propagated action potential and subsequent conduction blockade. This results in a transient and reversible loss of sensation in a localized area of the body.

Dyclonine hydrochloride is a white crystalline powder possessing topical anesthetic properties characterized by rapid onset of effect, lack of systemic toxicity and a low index of sensitization.

Dyclonine (536-43-6) is a topical anesthetic which has been used for oral and throat analgesia.1 Enhances neuronal mitochondrial function, potentiating respiration and providing protection against insults associated with neurodegenerative disorders.2 Inhibits aldehyde dehydrogenase ALDH3A1 resulting in accumulation of 4-hydroxynonenal, which renders head and neck squamous cell carcinoma cells sensitive to the cystine-glutamate antiporter inhibitor, sulfasalazine.3 Rescues frataxin deficiency in animal models as well as in buccal cells of patients with Friedreich’s Ataxia.4 Enhances the cytotoxic effect of proteasome inhibitors MG-1325 and bortezomib6 in cancer cells.

White Crystalline Solid

Dyclonine hydrochloride Basic Attributes

Molecular Weight：

325.87

Exact Mass：

325.18100

EC Number：

208-633-6

UNII：

ZEC193879Q

NSC Number：

756745|25588|23018

DSSTox ID：

DTXSID6045323

NCI Thesaurus Code：

C66875

Color/Form：

White

HScode：

2933399090

Characteristics

PSA：

29.54000

Melting Point：

175-176°C

Boiling Point：

424.5ºC at 760 mmHg

Flash Point：

210.5ºC

Water Solubility：

Partly soluble in water. Soluble in chloroform, ethanol, acetone and methanol.

Storage Conditions：

-20ºC Freezer

Collision Cross Section：

179.6 Å² [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

Critical Temperature & Pressure：

Inert atmosphere,2-8°C

Safety Information

Packing level：

III

Hazard category：

6.1(b)

Transport codes：

UN 3249

wgk germany：

hazard class code：

safety instructions：

26-36

RTECS Number：

UG8750000

Marks：

Precautionary statement(s)：

P261, P264, P270, P271, P280, P301+P310, P302+P352, P304+P340, P305+P351+P338, P310, P312, P321, P330, P332+P313, P362, P403+P233, P405, P501

Hazard Statements：

22-37/38-41

RIDADR：

3249

GHS Classification：

|Danger|H301 (97.44%): Toxic if swallowed [Danger Acute toxicity, oral]|P261, P264, P270, P271, P280, P301+P310, P302+P352, P304+P340, P305+P351+P338, P310, P312, P321, P330, P332+P313, P362, P403+P233, P405, and P501|Aggregated GHS information provided by 39 companies from 2 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Drug Information

MeSH：

Drugs that block nerve conduction when applied locally to nerve tissue in appropriate concentrations. They act on any part of the nervous system and on every type of nerve fiber. In contact with a nerve trunk, these anesthetics can cause both sensory and motor paralysis in the innervated area. Their action is completely reversible. (From Gilman AG, et. al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed) Nearly all local anesthetics act by reducing the tendency of voltage-dependent sodium channels to activate. (See all compounds classified as Anesthetics, Local.)

MeSH Entry Terms：

Dyclone

Dyclonine hydrochloride Use and Manufacturing

Methods of Manufacturing

The compound DYC was synthesized by the following reaction: DYC HCL was added to a solution of NaOH in H2O at r.t.. The mixture was stirred for 10 min, the water phase was extracted three times with EtOAc. The organic phase was dried over MgSO4, and concentrated. A light yellow liquid was obtained after the solvent were removed under reduced pressure (yield 87 %).

Uses

It is used for burns, abrasions, prurigo, insect bites, ulcers, bedsores, hemorrhoids, etc. It is also used for urinary tract and oral mucosal anesthesia.

Dyclonine hydrochloride is used for the temporary relief of the following occasional mouth and throat symptoms: pain, minor irritation, sore mouth and sore throat. It is a sodium channel blocker and a HSP90 chaperone protein inhibitor. It shows local anesthetic effects in vivo and is orally active.

Provides anesthesia of mucous membranes. Apply 5 to 10 minutes before a procedure; apply b.i.d. to t.i.d. for pain relief. Onset of action is within 2 to 10 minutes. Anesthesia lasts 30 to 60 minutes.

anesthetic (topical)

Used as a local anesthetic

Use Classification：

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:325.9
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:3
Rotatable Bond Count:8
Exact Mass:325.1808568
Monoisotopic Mass:325.1808568
Topological Polar Surface Area:29.5
Heavy Atom Count:22
Complexity:292
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes

Material

Formaldehyde

Sodium bromide

Downstream Products

Formaldehyde

Drug Function and Efficacy

It is a local anesthetic that has antipruritic and analgesic effects

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Dyclonine Chlorhexidine Sulfate Ointment
Ingredients	This product is a compound preparation, each gram contains 100 mg of sublimated sulfur, 5 mg of dyclonine hydrochloride, and 0.5 mg of chlorhexidine acetate.
Indication	1. This product should not come into contact with copper products to prevent deterioration. 2. This product can increase skin irritation and dryness when used with other acne treatment drugs, desquamation drugs, detergents, retinoic acid and other alcohol-containing preparations. 3. It should not be used with mercury-containing preparations, otherwise it can reduce the efficacy and increase irritation. 4. If used with other drugs at the same time, drug interactions may occur. Please consult a doctor or pharmacist for details.
Specifications	15%
Manufacturer	Shaanxi Xuelong Haimu Pude Pharmaceutical Co., Ltd.

Compound Dyclonine Mint Solution
Ingredients	This product is a compound preparation, each milliliter contains 5 mg of dyclonine hydrochloride, 320 mg of menthol, 30 mg of camphor, 260 mg of methyl salicylate, 30 mg of eucalyptus oil, 30 mg of eugenol, 100 mg of essential oil, and 1 mg of chlorophyll. Excipients are:
Indication	Drug interactions may occur if used with other drugs. Please consult your doctor or pharmacist for details.
Specifications	Compound
Manufacturer	Zhejiang Conba Pharmaceutical Co., Ltd.

Compound chlorhexidine dexamethasone membrane
Ingredients	This product is a compound preparation. Each patch contains 1.5 mg of chlorhexidine hydrochloride, 1 mg of vitamin B2, 0.05 mg of dexamethasone sodium phosphate, and 0.75 mg of dyclonine hydrochloride. Excipients include: polyvinyl alcohol, polysorbate 80, glycerin, and saccharin sodium.
Indication	1. Do not use other mouthwashes or oral medications at the same time when using this product; 2. If used with other drugs at the same time, drug interactions may occur. Please consult a doctor or pharmacist for details.
Specifications	Compound
Manufacturer	Guizhou Shenqi Pharmaceutical Co., Ltd.

See More Related Drugs

Registered Holders

APAC PHARMACEUTICAL LLC

United States
Active
Cavendish (Taizhou) Pharmaceutical Co., Ltd.

China
Active
Shandong Newtime Pharmaceutical Co., Ltd.

China
Active

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