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GUANFACINE HCL

GUANFACINE HCL structure

CAS No:
29110-48-3
Formula:
C9H9Cl2N3O.ClH
Chemical Name:
GUANFACINE HCL
Synonyms:
bs100-141;estulic;lon798;n-(aminoiminomethyl)-2,6-dichlorobenzeneacetamidehydrochloride;n-(aminoiminomethyl)-2,6-dichloro-benzeneacetamidmonohydrochloride;n-amidino-2-(2,6-dichlorophenyl)acetamidehydrochloride;N (AMINOIMINOMETHYL)-2,6-DICHLOROBENZENEACETAMIDE HYDROCHLORIDE SALT;[(2,6-DICHLOROPHENYL)ACETYL]GUANIDINE HYDROCHLORIDE
Categories:
Active Pharmaceutical Ingredients > Circulatory System Drugs

Description

Guanfacine Hcl, an anti-hypertensive agent, is a selective α2A-adrenoceptor agonist with Kd of 31 nM and displays 60-fold selectivity over α2B-adrenoceptors. IC50 Value: 31 nM(Kd)Target: Adrenergic ReceptorGuanfacine is a sympatholytic. It is a selective α2A receptor agonist. These receptors are concentrated heavily in the prefrontal cortex and the locus coeruleus, with the potential to improve attention resulting from interaction with receptors in the former. Guanfacine lowers both syst

Guanfacine hydrochloride is a member of acetamides. It has a role as a geroprotector.|Guanfacine Hydrochloride is the hydrochloride salt form of guanfacine, a centrally acting alpha-2 adrenergic agonist with antihypertensive activity. Alpha-2 receptor stimulation by guanfacine hydrochloride results in a decreased sympathetic outflow from the vasomotor center to the heart, kidneys, and peripheral vasculature. This leads to a decrease in heart rate and peripheral vascular resistance. (NCI05)|A centrally acting antihypertensive agent with specificity towards ADRENERGIC ALPHA-2 RECEPTORS.

ChEBI: Guanfacine hydrochloride is a member of acetamides. It has a role as a geroprotector.

Guanfacine hydrochloride,N-(aminoiminomethyl)-2,6-dichlorobenzeneacetamide(Tenex), is structurally related to clonidine hydrochloride andguanabenz acetate and shares many of their pharmacologicalproperties. The drug has a longer duration of action than eitherclonidine hydrochloride or guanabenz acetate. It lasts upto 24 hours. It also requires much longer (8–12 hours) for apeak effect to occur after the drug is administered.

GUANFACINE HCL Basic Attributes

Molecular Weight：

282.55

Exact Mass：

280.988953

EC Number：

249-443-3

UNII：

PML56A160O

NSC Number：

759121

DSSTox ID：

DTXSID2045157

NCI Thesaurus Code：

C47550

Color/Form：

white

ATC Code：

C02AC02

HScode：

2925294500

Characteristics

PSA：

81.5

XLogP3：

3.53850

Appearance：

white

Melting Point：

215-217℃

Water Solubility：

H2O: soluble 12mg/mL at60°C

Storage Conditions：

Store at RT

Toxicity：

LD50 in mice: 165 mg/kg orally (Coward)

Critical Temperature & Pressure：

Inert atmosphere,Room Temperature

Safety Information

Packing level：

III

Hazard category：

6.1(b)

Transport codes：

3249

wgk germany：

hazard class code：

6.1

RTECS Number：

CY1481000

Storage features：

Store at RT

Precautionary statement(s)：

P201, P202, P260, P263, P264, P270, P281, P301+P310, P308+P313, P321, P330, P405, P501

Hazard Statements：

H301

RIDADR：

3249

GHS Classification：

|Danger|H301 (100%): Toxic if swallowed [Danger Acute toxicity, oral]|P201, P202, P264, P270, P281, P301+P310, P308+P313, P321, P330, P405, and P501|Aggregated GHS information provided by 11 companies from 3 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Drug Information

Drug Indication：

Treatment of attention deficit hyperactivity disorder (ADHD) in children and adolescents 6 to 17 years old for whom stimulants are not suitable, not tolerated or have been shown to be ineffective.Intuniv must be used as a part of a comprehensive ADHD treatment programme, typically including psychological, educational and social measures.|Treatment of Attention Deficit Hyperactivity Disorder (ADHD)

MeSH：

Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS. (See all compounds classified as Antihypertensive Agents.)|Compounds that bind to and activate ADRENERGIC ALPHA-2 RECEPTORS. (See all compounds classified as Adrenergic alpha-2 Receptor Agonists.)

MeSH Entry Terms：

BS 100 141

GUANFACINE HCL Use and Manufacturing

Methods of Manufacturing

A solution of methyl 2-(2, 6-dichlorophenyl)acetate (75 mg, 0.26 mmol) in ethanol (3 mL) was added to a solution of guanidine hydrochloride (25 mg, 0.26 mmol) and sodium ethoxide (6.0 mg of sodium in 2 mL methanol). The prepared guanfacine crude was dissolved in 700ml 95percent ethanol, the insoluble material was filtered off. Concentrated hydrochloric acid was added to the filtrate until pH = 1, stirring for 30 min. With a rotary evaporator, at 50 ° C, a vacuum of 0.085Mpa, 60percent solvent was concentrated to remove the remaining cooling To 30 ° C, crystallization 3 hours, filtered to give crude guanfacine hydrochloride Compound 53g;The guanfacine hydrochloride crude was dissolved in 550ml of 95percent ethanol, heated to reflux, filtered hot, the filtrate was cooled to 30 , crystallization 2Hour, filtered, dried at 105 for 5 hours to obtain a finished product 32.6 g.

Uses

Antihypertensor;Alpha 2A agonist

Guanfacine hydrochloride may be used as a pharmaceutical reference standard for the determination of the analyte in bulk drug and pharmaceutical formulations by spectrophotometry and high performance liquid chromatography.

Centrally acting a-adrenoceptor agonist. Antihypertensive

Use Classification：

Human drugs -> Intuniv -> EMA Drug Category|Antiadrenergic agents, centrally acting, Antihypertensives -> Human pharmacotherapeutic group|Human Drugs -> EU pediatric investigation plans|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:282.5
Hydrogen Bond Donor Count:3
Hydrogen Bond Acceptor Count:1
Rotatable Bond Count:2
Exact Mass:280.988945
Monoisotopic Mass:280.988945
Topological Polar Surface Area:81.5
Heavy Atom Count:16
Complexity:256
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes

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n-(aminoiminomethyl)-2,6-dichlorobenzeneacetamidehydrochloride;n-(aminoiminomethyl)-2,6-dichloro-benzeneacetamidmonohydrochloride;n-amidino-2-(2,6-dic

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Guanfacine HCl CAS No.29110-48-3

CAS No.: 29110-48-3

Grade: Pharmaceutical grade

Content: 99%

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