RX821002 HCl | CAS#109544-45-8 | α2-adrenoceptor antagonist

MedKoo Cat#: 532602 | Name: RX821002 HCl

Description:

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

RX821002 is a potent, selective α2-adrenoceptor antagonist with very low affinity for imidazoline sites. RX821002 displays selectivity for the α2D over the α2A subtypes (pKd values are 9.7 and 8.2 respectively).

Chemical Structure

RX821002 HCl

CAS#109544-45-8 (HCl)

Theoretical Analysis

MedKoo Cat#: 532602

Name: RX821002 HCl

CAS#: 109544-45-8 (HCl)

Chemical Formula: C12H15ClN2O3

Exact Mass: 0.0000

Molecular Weight: 270.71

Elemental Analysis: C, 53.24; H, 5.59; Cl, 13.10; N, 10.35; O, 17.73

Price and Availability

Size	Price	Availability
50mg	USD 250.00	2 Weeks
100mg	USD 450.00	2 Weeks
200mg	USD 750.00	2 Weeks
500mg	USD 1,450.00	2 Weeks
1g	USD 2,250.00	2 Weeks
2g	USD 3,850.00	2 Weeks

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Related CAS #

109544-45-8 (HCl) 102575-24-6 (free base)

Synonym

RX821002; RX 821002; RX-821002; RX821002 HCl; RX821002 hydrochloride;

IUPAC/Chemical Name

2-(2,3-Dihydro-2-methoxy-1,4-benzodioxin-2-yl)-4,5-dihydro-1H-imidazole hydrochloride

InChi Key

IMPOOMVZVWKSAP-UHFFFAOYSA-N

InChi Code

InChI=1S/C12H14N2O3.ClH/c1-15-12(11-13-6-7-14-11)8-16-9-4-2-3-5-10(9)17-12;/h2-5H,6-8H2,1H3,(H,13,14);1H

SMILES Code

COC1(C2=NCCN2)OC3=CC=CC=C3OC1.[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:

RX821002 displays selectivity for the α2D over the α2A subtypes (pKd values are 9.7 and 8.2 respectively).

In vitro activity:

When compared to [3H]rauwolscine, RX 821002 exhibited reduced nonspecific binding and higher affinity in most cases. RX 821002 consistently detected more alpha-2 adrenoceptors in specific tissues and cells, including rat cerebral cortex, spleen, guinea pig kidney, human platelets, and HEL cells. The findings support the notion that RX 821002 is a more suitable ligand for alpha-2 adrenoceptor detection due to its favorable binding characteristics and specificity. Reference: J Pharmacol Exp Ther. 1995 Jun;273(3):1287-94. https://pubmed.ncbi.nlm.nih.gov/7791100/

In vivo activity:

This study used rats with neonatal ventral hippocampal lesions (NVHL) as a schizophrenia model. Both RX821002 and caffeine increased locomotion, particularly in NVHL rats, but RX821002 exhibited a biphasic effect initially reducing and then enhancing locomotion. RX821002 also improved learning in NVHL rats, while caffeine had no significant impact on learning. RX821002 may hold promise in mitigating cognitive deficits associated with schizophrenia.. Reference: Front Behav Neurosci. 2014 Jan 28;8:15. https://pubmed.ncbi.nlm.nih.gov/24478661/

	Solvent	mg/mL	mM
Solubility
	DMSO	27.1	100.00

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 270.71 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. Díez-Alarcia R, Pilar-Cuéllar F, Paniagua MA, Meana JJ, Fernández-López A. Pharmacological characterization and autoradiographic distribution of alpha2-adrenoceptor antagonist [3H]RX 821002 binding sites in the chicken brain. Neuroscience. 2006 Aug 11;141(1):357-69. doi: 10.1016/j.neuroscience.2006.03.025. Epub 2006 May 11. PMID: 16697114. 2. Erdbrügger W, Raulf M, Otto T, Michel MC. Does [3H]2-methoxy-idazoxan (RX 821002) detect more alpha-2-adrenoceptor agonist high-affinity sites than [3H]rauwolscine? A comparison of nine tissues and cell lines. J Pharmacol Exp Ther. 1995 Jun;273(3):1287-94. PMID: 7791100. 3. Chu X, Ågmo A. The adrenergic α2-receptor, sexual incentive motivation and copulatory behavior in the male rat. Pharmacol Biochem Behav. 2016 May;144:33-44. doi: 10.1016/j.pbb.2016.02.008. Epub 2016 Feb 22. PMID: 26906229. 4. Sandner G, Angst MJ, Guiberteau T, Guignard B, Nehlig A. Effects of caffeine or RX821002 in rats with a neonatal ventral hippocampal lesion. Front Behav Neurosci. 2014 Jan 28;8:15. doi: 10.3389/fnbeh.2014.00015. PMID: 24478661; PMCID: PMC3904090.

In vitro protocol:

In vivo protocol:

1. Chu X, Ågmo A. The adrenergic α2-receptor, sexual incentive motivation and copulatory behavior in the male rat. Pharmacol Biochem Behav. 2016 May;144:33-44. doi: 10.1016/j.pbb.2016.02.008. Epub 2016 Feb 22. PMID: 26906229. 2. Sandner G, Angst MJ, Guiberteau T, Guignard B, Nehlig A. Effects of caffeine or RX821002 in rats with a neonatal ventral hippocampal lesion. Front Behav Neurosci. 2014 Jan 28;8:15. doi: 10.3389/fnbeh.2014.00015. PMID: 24478661; PMCID: PMC3904090.

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