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GUANFACINE HCL

Product Name
GUANFACINE HCL
CAS No.
29110-48-3
Chemical Name
GUANFACINE HCL
Synonyms
GUANFACINE HYDROCHLORIDE;Tenex;Intuniv;lon798;estulic;bs100-141;Guarfacine;Guanfascine;GUANFACINE HCL;Guanfacine HCL powder
CBNumber
CB0767424
Molecular Formula
C9H9Cl2N3O.ClH
Formula Weight
282.55
MOL File
29110-48-3.mol
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GUANFACINE HCL Property

Melting point:
215-217℃
RTECS 
CY1481000
storage temp. 
Inert atmosphere,Room Temperature
solubility 
H2O: 12 mg/mL at 60 °C, soluble
form 
Solid
color 
white
Merck 
14,4561
Stability:
Hygroscopic
InChIKey
DGFYECXYGUIODH-UHFFFAOYSA-N
CAS DataBase Reference
29110-48-3(CAS DataBase Reference)
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Safety

RIDADR 
3249
WGK Germany 
3
HazardClass 
6.1(b)
PackingGroup 
III
HS Code 
2925294500
Toxicity
LD50 in mice: 165 mg/kg orally (Coward)
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H301Toxic if swalloed

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P321Specific treatment (see … on this label).

P405Store locked up.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
G1043
Product name
Guanfacine hydrochloride
Purity
≥98% (HPLC)
Packaging
10mg
Price
$62.9
Updated
2024/03/01
Sigma-Aldrich
Product number
1302101
Product name
Guanfacine hydrochloride
Purity
United States Pharmacopeia (USP) Reference Standard
Packaging
125mg
Price
$358
Updated
2024/03/01
TCI Chemical
Product number
G0414
Product name
Guanfacine Hydrochloride
Purity
>98.0%(HPLC)(T)
Packaging
100mg
Price
$69
Updated
2024/03/01
TCI Chemical
Product number
G0414
Product name
Guanfacine Hydrochloride
Purity
>98.0%(HPLC)(T)
Packaging
1g
Price
$438
Updated
2024/03/01
Alfa Aesar
Product number
J67086
Product name
Guanfacine hydrochloride, 99%
Packaging
10mg
Price
$105
Updated
2021/12/16
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GUANFACINE HCL Chemical Properties,Usage,Production

Originator

Estulic,Sandoz,Switz.,1980

Uses

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.

Uses

Antihypertensor;Alpha 2A agonist

Uses

Centrally acting a-adrenoceptor agonist. Antihypertensive

Definition

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

Manufacturing Process

2,6-Dichlorophenyl-acetyl-guanidine: A solution of 3.245 g (0.055 mol) of guanidine in isopropanol is added to a solution of 11.7 g (0.05 mol) of 2,6- dichlorophenyl-acetic acid ethyl ester (BP 142°C to 143°C/12 mm of Hg) in 20cc of isopropanol. The reaction mixture is allowed to stand overnight and is subsequently concentrated by evaporation. After recrystallizing the residue from methanol/ether 2,6-dichlorophenyl-acetyl-guanidine is obtained in the form of white grains having a MP of 225°C to 227°C.
2,6-Dichlorophenyl-acetyl-guanidine hydrochloride: A solution of 5.6 g (0.025 mol) of 2,-dichlorophenylacetic acid chloride (BP 137°C to 138°C/12 mm of Hg) in 10 cc of toluene is added dropwise to a mixture of 4.5 g (0.076 mol) of guanidine and 60 cc of toluene. The reaction mixture is allowed to stand at room temperature for 20 minutes, is then heated on a steam bath for 2 hours and is subsequently cooled. The resulting precipitate is filtered off and washed twice with 25 cc amounts of water in order to separate the guanidine hydrochloride. The residue (2,6-dichlorophenyl-acetyl-guanidine) is washed with chloroform for further purification and is then dissolved in 50 cc of isopropanol. The pH-value of the solution is adjusted to 6 with ethanolic hydrochloric acid and the solution is cooled. The resulting white needles are again washed with chloroform. The resulting 2.6-dichlorophenyl-acetylguanidine hydrochloride has a MP of 213°C to 216°C.

brand name

Tenex (Dr. Reddy’s).

Therapeutic Function

Antihypertensive

General Description

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.

Biological Activity

Selective α 2A -adrenoceptor agonist (K d = 31 nM). Displays 60-fold selectivity over α 2B -adrenoceptors. Also available as part of the α 2 -Adrenoceptor Tocriset™ .

Biochem/physiol Actions

α-2 noradrenergic receptor agonist.

Pharmacokinetics

The pharmacokinetic properties for guanfacine differ from those of clonidine, guanabenz, and α-methyldopa. At pH 7.4, guanfacine is predominately (67%) in the nonionized, lipid-soluble base form, which accounts for its high oral bioavailability (>80%). Following an oral dose, peak plasma concentrations occur in 1 to 4 hours, with a relatively long elimination half-life of 14 to 23 hours. The maximum blood pressure response occurs in 8 to 12 hours after oral administration and is maintained up to 36 hours following its discontinuation. Following IV dosing, guanfacine achieves the highest concentrations in liver and kidney, with low concentrations in the brain. Guanfacine is 64% bound to plasma proteins. In patients with hepatic or renal impairment, its elimination half-life may be prolonged.
Guanfacine is metabolized principally by hepatic hydroxylation to its inactive metabolite, 3-hydroxyguanfacine (20%), which is eliminated in the urine as its glucuronide (30%), sulfate (8%), or mercapturic acid conjugate (10%), and 24 to 37% is excreted as unchanged guanfacine. Its nearly complete bioavailability suggests no evidence of any first-pass effect. Guanfacine and its inactive metabolites are excreted principally in urine, with approximately 80% of its oral dose excreted in urine within 48 hours.

Clinical Use

Overall, the therapeutic applications for guanfacine are similar to those of the other centrally acting α2-adrenergic agonists and methyldopa. It has been effective as monotherapy in the treatment of patients with mild to moderate hypertension. One advantage for guanfacine is its once-a-day dosing schedule. The use of diuretics to prevent accumulation of fluid may allow a reduction in the dosage for guanfacine.

Side effects

Overall, although the frequency of troublesome adverse effects produced by guanfacine is similar to that produced by clonidine and the other centrally acting sympatholytics, their incidence and severity are lower with guanfacine. Unlike clonidine, abrupt discontinuation of guanfacine rarely results in rebound hypertension. When a withdrawal syndrome has occurred, its onset was slower and its symptoms less severe than the syndrome observed with clonidine.

storage

Store at RT

GUANFACINE HCL Preparation Products And Raw materials

Raw materials

Preparation Products

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GUANFACINE HCL Suppliers

PROCOS SPA
Tel
--
Fax
--
Email
info@procos.it
Country
Italy
ProdList
20
Advantage
58
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View Lastest Price from GUANFACINE HCL manufacturers

Wuhan Nutra Biotechnology Co.,Ltd
Product
Guanfacine hydrochloride 29110-48-3
Price
US $30.00-0.00/g
Min. Order
1g
Purity
98%+
Supply Ability
100kgs
Release date
2021-05-19
Hebei Yanxi Chemical Co., Ltd.
Product
GUANFACINE HCL 29110-48-3
Price
US $40.00/kg
Min. Order
1kg
Purity
0.99
Supply Ability
10 tons
Release date
2023-09-25
Hebei Chuanghai Biotechnology Co,.LTD
Product
Guanfacine HCL powder 29110-48-3
Price
US $1.90/KG
Min. Order
1KG
Purity
99%
Supply Ability
10 ton
Release date
2024-08-15

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