Guanfacine HCl | CAS#29110-48-3

MedKoo Cat#: 326782 | Name: Guanfacine HCl

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Guanfacine, also known as BS 100-141 and SPD-503, is a sympatholytic drug used in the treatment of attention deficit hyperactivity disorder (ADHD) and hypertension (not to be confused with guaifenesin, an expectorant). 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 systolic and diastolic blood pressure by activating the central nervous system α2A norepinephrine autoreceptors, which results in reduced peripheral sympathetic outflow and thus a reduction in peripheral sympathetic tone. Guanfacine is currently approved and marketed in the United States[8] and Europe[9] as Intuniv for the treatment of ADHD in children and adolescents aged 6–18 years.

Chemical Structure

Guanfacine HCl

CAS#29110-48-3 (HCl)

Theoretical Analysis

MedKoo Cat#: 326782

Name: Guanfacine HCl

CAS#: 29110-48-3 (HCl)

Chemical Formula: C9H10Cl3N3O

Exact Mass: 0.0000

Molecular Weight: 282.55

Elemental Analysis: C, 38.26; H, 3.57; Cl, 37.64; N, 14.87; O, 5.66

Price and Availability

Size	Price	Availability
100mg	USD 250.00	2 Weeks
200mg	USD 350.00	2 Weeks
500mg	USD 650.00	2 Weeks
1g	USD 950.00	2 Weeks

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Related CAS #

29110-48-3 (HCl) 29110-47-2 (free base)

Synonym

Guanfacine Hydrochloride; Guanfacine HCl; BS 100-141; BS-100-141; BS100-141; SPD-503; SPD 503; SPD503;

IUPAC/Chemical Name

N-(Aminoiminomethyl)-2,6-dichlorobenzeneacetamide Hydrochloride

InChi Key

DGFYECXYGUIODH-UHFFFAOYSA-N

InChi Code

InChI=1S/C9H9Cl2N3O.ClH/c10-6-2-1-3-7(11)5(6)4-8(15)14-9(12)13;/h1-3H,4H2,(H4,12,13,14,15);1H

SMILES Code

O=C(NC(N)=N)CC1=C(Cl)C=CC=C1Cl.[H]Cl

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

Guanfacine hydrochloride, 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)

In vitro activity:

TBD

In vivo activity:

The results indicate that guanfacine improved poor noradrenergic modulation of neuronal circuits that involve the frontal lobes in an animal rat model of ADHD. The present results support the beneficial effects of guanfacine on ADHD behavior reported clinically and experimentally in primate models of frontal function. Reference: Behav Brain Funct. 2006 Dec 15;2:41. https://pubmed.ncbi.nlm.nih.gov/17173664/

	Solvent	mg/mL	mM
Solubility
	DMF	30.0	106.18
	DMSO	36.1	127.64
	Ethanol	40.5	143.34
	PBS (pH 7.2)	10.0	35.39
	Water	26.1	92.33

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 282.55 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Sagvolden T. The alpha-2A adrenoceptor agonist guanfacine improves sustained attention and reduces overactivity and impulsiveness in an animal model of Attention-Deficit/Hyperactivity Disorder (ADHD). Behav Brain Funct. 2006 Dec 15;2:41. doi: 10.1186/1744-9081-2-41. PMID: 17173664; PMCID: PMC1764416. 2. Arnsten AF, Cai JX, Goldman-Rakic PS. The alpha-2 adrenergic agonist guanfacine improves memory in aged monkeys without sedative or hypotensive side effects: evidence for alpha-2 receptor subtypes. J Neurosci. 1988 Nov;8(11):4287-98. doi: 10.1523/JNEUROSCI.08-11-04287.1988. PMID: 2903226; PMCID: PMC6569464.

In vitro protocol:

TBD

In vivo protocol:

1: Guanfacine Hydrochloride Extended Release (Intuniv XR) Tablets: For the Treatment of Attention-Deficit/Hyperactivity Disorder [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2015 Jul. Available from http://www.ncbi.nlm.nih.gov/books/NBK349448/ PubMed PMID: 26962601. 2: Bello NT. Clinical utility of guanfacine extended release in the treatment of ADHD in children and adolescents. Patient Prefer Adherence. 2015 Jun 30;9:877-85. doi: 10.2147/PPA.S73167. eCollection 2015. Review. PubMed PMID: 26170637; PubMed Central PMCID: PMC4494608. 3: Martinez-Raga J, Knecht C, de Alvaro R. Profile of guanfacine extended release and its potential in the treatment of attention-deficit hyperactivity disorder. Neuropsychiatr Dis Treat. 2015 May 28;11:1359-70. doi: 10.2147/NDT.S65735. eCollection 2015. Review. PubMed PMID: 26064054; PubMed Central PMCID: PMC4455846. 4: Rizzo R, Martino D. Guanfacine for the treatment of attention deficit hyperactivity disorder in children and adolescents. Expert Rev Neurother. 2015 Apr;15(4):347-54. doi: 10.1586/14737175.2015.1028370. Review. PubMed PMID: 25800130. 5: Ruggiero S, Clavenna A, Reale L, Capuano A, Rossi F, Bonati M. Guanfacine for attention deficit and hyperactivity disorder in pediatrics: a systematic review and meta-analysis. Eur Neuropsychopharmacol. 2014 Oct;24(10):1578-90. doi: 10.1016/j.euroneuro.2014.08.001. Epub 2014 Aug 11. Review. PubMed PMID: 25156577. 6: Connor DF, Arnsten AF, Pearson GS, Greco GF. Guanfacine extended release for the treatment of attention-deficit/hyperactivity disorder in children and adolescents. Expert Opin Pharmacother. 2014 Aug;15(11):1601-10. doi: 10.1517/14656566.2014.930437. Epub 2014 Jul 3. Review. PubMed PMID: 24992513. 7: Fox H, Sinha R. The role of guanfacine as a therapeutic agent to address stress-related pathophysiology in cocaine-dependent individuals. Adv Pharmacol. 2014;69:217-65. doi: 10.1016/B978-0-12-420118-7.00006-8. Review. PubMed PMID: 24484979; PubMed Central PMCID: PMC4017947. 8: Faraone SV, McBurnett K, Sallee FR, Steeber J, López FA. Guanfacine extended release: a novel treatment for attention-deficit/hyperactivity disorder in children and adolescents. Clin Ther. 2013 Nov;35(11):1778-93. doi: 10.1016/j.clinthera.2013.09.005. Epub 2013 Oct 16. Review. PubMed PMID: 24139092. 9: Bukstein OG, Head J. Guanfacine ER for the treatment of adolescent attention-deficit/hyperactivity disorder. Expert Opin Pharmacother. 2012 Oct;13(15):2207-13. doi: 10.1517/14656566.2012.721778. Epub 2012 Sep 7. Review. PubMed PMID: 22957772. 10: Childress AC. Guanfacine extended release as adjunctive therapy to psychostimulants in children and adolescents with attention-deficit/hyperactivity disorder. Adv Ther. 2012 May;29(5):385-400. doi: 10.1007/s12325-012-0020-1. Epub 2012 May 18. Review. PubMed PMID: 22610723. 11: Arnsten AF, Jin LE. Guanfacine for the treatment of cognitive disorders: a century of discoveries at Yale. Yale J Biol Med. 2012 Mar;85(1):45-58. Epub 2012 Mar 29. Review. PubMed PMID: 22461743; PubMed Central PMCID: PMC3313539. 12: Sallee FR, Eaton K. Guanfacine extended-release for attention-deficit/hyperactivity disorder (ADHD). Expert Opin Pharmacother. 2010 Oct;11(15):2549-56. doi: 10.1517/14656566.2010.517523. Review. PubMed PMID: 20831361. 13: Muir VJ, Perry CM. Guanfacine extended-release: in attention deficit hyperactivity disorder. Drugs. 2010 Sep 10;70(13):1693-702. doi: 10.2165/11205940-000000000-00000. Review. PubMed PMID: 20731476. 14: Connor DF, Rubin J. Guanfacine extended release in the treatment of attention deficit hyperactivity disorder in children and adolescents. Drugs Today (Barc). 2010 May;46(5):299-314. doi: 10.1358/dot.2010.46.5.1450095. Review. PubMed PMID: 20517532. 15: Posey DJ, McDougle CJ. Guanfacine and guanfacine extended release: treatment for ADHD and related disorders. CNS Drug Rev. 2007 Winter;13(4):465-74. Review. PubMed PMID: 18078429. 16: King A, Harris P, Fritzell J, Kurlan R. Syncope in children with Tourette's syndrome treated with guanfacine. Mov Disord. 2006 Mar;21(3):419-20. Review. PubMed PMID: 16229000. 17: Eliseev OM. [The new antihypertensive preparation guanfacine (Estulic)]. Ter Arkh. 1992;64(9):103-12. Review. Russian. PubMed PMID: 1481145. 18: Mosqueda-Garcia R. Guanfacine: a second generation alpha 2-adrenergic blocker. Am J Med Sci. 1990 Jan;299(1):73-6. Review. PubMed PMID: 1967513. 19: Cornish LA. Guanfacine hydrochloride: a centrally acting antihypertensive agent. Clin Pharm. 1988 Mar;7(3):187-97. Review. PubMed PMID: 3281788. 20: Sorkin EM, Heel RC. Guanfacine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in the treatment of hypertension. Drugs. 1986 Apr;31(4):301-36. Review. PubMed PMID: 3519177.