RJR 2429 (dihydrochloride) | AChR Agonist | CAS#1021418-53-0

MedKoo Cat#: 471051 | Name: RJR 2429 dihydrochloride

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Description:

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

RJR 2429 dihydrochloride is a nicotinic acetylcholine receptor (AChR) agonist that displays selectivity for α4β2.

Chemical Structure

RJR 2429 dihydrochloride

CAS#1021418-53-0

Theoretical Analysis

MedKoo Cat#: 471051

Name: RJR 2429 dihydrochloride

CAS#: 1021418-53-0

Chemical Formula: C12H18Cl2N2

Exact Mass:

Molecular Weight: 261.19

Elemental Analysis: C, 55.18; H, 6.95; Cl, 27.14; N, 10.73

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 250.00
10mg	USD 340.00
25mg	USD 800.00

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Synonym

RJR 2429 dihydrochloride, RJR2429 dihydrochloride, RJR-2429 dihydrochloride, RJR 2429 2HCl, RJR 2429 HCl

IUPAC/Chemical Name

2-(3-pyridinyl)-1-azabicyclo[2.2.2]octane, dihydrochloride

InChi Key

PIUNXHHZRIUBOV-UHFFFAOYSA-N

InChi Code

InChI=1S/C12H16N2.2ClH/c1-2-11(9-13-5-1)12-8-10-3-6-14(12)7-4-10;;/h1-2,5,9-10,12H,3-4,6-8H2;2*1H

SMILES Code

[H]Cl.[H]Cl.N1(CC2)C(C3=CC=CN=C3)CC2CC1

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 and water

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO and water

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

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Product Data

Product Data

Instruction

View handling instruction

Biological target:

RJR 2429 dihydrochloride is a potent nAChR agonist that displays selectivity for α4β2 (Ki = 1 nM) and α1βγδ subtypes (EC50 values 297 and 55 nM, respectively). RJR 2429 dihydrochloride induces dopamine release from striatal neurons (EC50 = 2 nM) and inhibits ion flux in thalamic neurons (IC50 = 154 nM). It is a putative α3β4 agonist that potentiates catecholamine release.

In vitro activity:

RJR-2429 is less potent in activating nAChRs in the clonal cell line PC12, with EC50 = 1100 +/- 230 nM and Emax = 85 +/- 20% when compared with nicotine. The activation of a putative alpha 3 beta 4-containing nAChR in PC12 by RJR-2429 reveals a potency intermediate between nicotine and epibatidine (EC50 of 20,000 nM for nicotine and 30 nM for epibatidine). Reference: J Pharmacol Exp Ther. 1998 Mar;284(3):886-94. https://pubmed.ncbi.nlm.nih.gov/9495846/

In vivo activity:

This study characterized nicotinic acetylcholine receptors involved in the release of catecholamines from the rat adrenal gland. The efficacies of these agonists are as follows: (+/-) epibatidine >> RJR-2429>(-)-cytisine>(-)-nicotine >> RJR-2403. These results suggest that alpha3beta4 nicotinic receptors are involved in the release of catecholamines from the rat adrenal gland. Reference: Eur J Pharmacol. 2002 Jun 20;446(1-3):83-7. https://pubmed.ncbi.nlm.nih.gov/12098588/

	Solvent	mg/mL	mM
Solubility
	DMSO	100.0	382.86
	Water	100.0	382.86

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 261.19 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. Bhatti BS, Strachan JP, Breining SR, Miller CH, Tahiri P, Crooks PA, Deo N, Day CS, Caldwell WS. Synthesis of 2-(pyridin-3-yl)-1-azabicyclo[3.2.2]nonane, 2-(pyridin-3-yl)-1-azabicyclo[2.2.2]octane, and 2-(pyridin-3-yl)-1-azabicyclo[3.2.1]octane, a class of potent nicotinic acetylcholine receptor-ligands. J Org Chem. 2008 May 2;73(9):3497-507. doi: 10.1021/jo800028q. Epub 2008 Mar 26. PMID: 18363376. 2. Bencherif M, Schmitt JD, Bhatti BS, Crooks P, Caldwell WS, Lovette ME, Fowler K, Reeves L, Lippiello PM. The heterocyclic substituted pyridine derivative (+/-)-2-(-3-pyridinyl)-1-azabicyclo[2.2.2]octane (RJR-2429): a selective ligand at nicotinic acetylcholine receptors. J Pharmacol Exp Ther. 1998 Mar;284(3):886-94. PMID: 9495846. 3. Yokotani K, Okada S, Nakamura K. Characterization of functional nicotinic acetylcholine receptors involved in catecholamine release from the isolated rat adrenal gland. Eur J Pharmacol. 2002 Jun 20;446(1-3):83-7. doi: 10.1016/s0014-2999(02)01819-8. PMID: 12098588.

In vitro protocol:

In vivo protocol:

1. Yokotani K, Okada S, Nakamura K. Characterization of functional nicotinic acetylcholine receptors involved in catecholamine release from the isolated rat adrenal gland. Eur J Pharmacol. 2002 Jun 20;446(1-3):83-7. doi: 10.1016/s0014-2999(02)01819-8. PMID: 12098588.

1. Playa, H.et al. Dilazep analogues for the study of equilibrative nucleoside transporters 1 and 2 (ENT1 and ENT2). Bioorg. Med. Chem. Lett. 2014, 24(24), 5801-5804. 2. Bhatti, B.et al.Synthesis of 2-(pyridin-3-yl)-1-azabicyclo[3.2.2]nonane, 2-(pyridin-3-yl)-1-azabicyclo[2.2.2]octane, and 2-(pyridin-3-yl)-1-azabicyclo[3.2.1]octane, a class of potent nicotinic acetylcholine receptor-ligands. J. Org. Chem. 2008, 73(9), 3497-3507. 3. Yokotani K. et al Characterization of functional nicotinic acetylcholine receptors involved in catecholamine release from isolated rat adrenal gland. Eur.J.Pharmacol. 2002, 446(1-3):83-7 4. Bencherif, M. et al. The heterocyclic substituted pyridine derivative (+/-)-2-(-3-pyridinyl)-1-azabicyclo[2.2.2]octane (RJR-2429): A selective ligand at nicotinic acetylcholine receptors. J. Pharmacol. Exp. Ther. 1998, 284(3), 886-894