Varenicline HCl

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MedKoo CAT#: 463313

CAS#: 866823-63-4 (HCl)

Description: Varenicline is a nicotinic receptor partial agonist—it stimulates nicotine receptors more weakly than nicotine itself does. In this respect it is similar to cytisine and different from the nicotinic antagonist, bupropion, and nicotine replacement therapies (NRTs) like nicotine patches and nicotine gum. Varenicline displays full agonism on α7 nicotinic acetylcholine receptors and is a partial agonist on the α4β2, α3β4, and α6β2 subtypes. In addition, it is a weak agonist on the α3β2 containing receptors. Varenicline's partial agonism on the α4β2 receptors rather than nicotine's full agonism produces less effect of dopamine release than nicotine's. This α4β2 competitive binding reduces the ability of nicotine to bind and stimulate the mesolimbic dopamine system—similar to the method of action of buprenorphine in the treatment of opioid addiction.

Chemical Structure

Varenicline HCl
CAS# 866823-63-4 (HCl)

Theoretical Analysis

MedKoo Cat#: 463313
Name: Varenicline HCl
CAS#: 866823-63-4 (HCl)
Chemical Formula: C13H15Cl2N3
Exact Mass: 283.0643
Molecular Weight: 284.184
Elemental Analysis: C, 54.94; H, 5.32; Cl, 24.95; N, 14.79

Price and Availability

Size Price Availability Quantity
25.0mg USD 250.0 2 Weeks
50.0mg USD 450.0 2 Weeks
100.0mg USD 750.0 2 Weeks
200.0mg USD 1250.0 2 Weeks
500.0mg USD 2050.0 2 Weeks
1.0g USD 2950.0 2 Weeks
2.0g USD 5150.0 2 Weeks
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Related CAS #: 375815-87-5 (tartrate)   866823-63-4 (HCl)   249296-44-4 (free base)    

Synonym: Varenicline dihydrochloride; HSDB7591; HSDB-7591; HSDB 7591; CP 526555; CP-526555; CP526555;

IUPAC/Chemical Name: 7,8,9,10-tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline dihydrochloride


InChi Code: InChI=1S/C13H13N3.2ClH/c1-2-16-13-5-11-9-3-8(6-14-7-9)10(11)4-12(13)15-1;;/h1-2,4-5,8-9,14H,3,6-7H2;2*1H

SMILES Code: [H]Cl.[H]Cl.C12=CC(C3CNCC4C3)=C4C=C1N=CC=N2

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: >3 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

Preparing Stock Solutions

The following data is based on the product molecular weight 284.184 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.

Recalculate based on batch purity %
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

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1: Lynch KG, Plebani J, Spratt K, Morales M, Tamminga M, Feibush P, Kampman KM. Varenicline for the Treatment of Cocaine Dependence. J Addict Med. 2021 Apr 8. doi: 10.1097/ADM.0000000000000842. Epub ahead of print. PMID: 33840773.

2: Walker N, Smith B, Barnes J, Verbiest M, Parag V, Pokhrel S, Wharakura MK, Lees T, Cubillos Gutierrez H, Jones B, Bullen C. Cytisine versus varenicline for smoking cessation in New Zealand indigenous Māori: A randomized controlled trial. Addiction. 2021 Mar 24. doi: 10.1111/add.15489. Epub ahead of print. PMID: 33761149.

3: Svendsen M, Heggen E, Klemsdal TO, Tonstad S. Diet, eating behaviour and weight gain in men and women with overweight/obesity receiving varenicline for smoking cessation. Clin Obes. 2021 Mar 9:e12447. doi: 10.1111/cob.12447. Epub ahead of print. PMID: 33751845.

4: Russo C, Caponnetto P, Cibella F, Maglia M, Alamo A, Campagna D, Frittitta L, Di Mauro M, Leotta C, Mondati E, Krysiński A, Franek E, Polosa R. A double blind randomized controlled trial investigating efficacy and safety of varenicline for smoking cessation in patients with type 2 diabetes: study protocol. Intern Emerg Med. 2021 Mar 18. doi: 10.1007/s11739-021-02684-1. Epub ahead of print. PMID: 33735416.

5: Chenoweth MJ, Lerman C, Knight J, Tyndale RF. A genome-wide association study of nausea incidence in varenicline-treated cigarette smokers. Nicotine Tob Res. 2021 Mar 13:ntab044. doi: 10.1093/ntr/ntab044. Epub ahead of print. PMID: 33713409.

6: Kim E, Hwang JG, Park SJ, Han JY, Choi YS, Park SR, Yu KS, Park MK, Lee S. Pharmacokinetic comparison between tablet of varenicline tartrate and orally disintegrating film of varenicline salicylate in healthy subjects. Int J Clin Pharmacol Ther. 2021 Mar 11. doi: 10.5414/CP203953. Epub ahead of print. PMID: 33704052.

7: Fucito LM, Wu R, O'Malley SS, Hanrahan TH, Ikomi JT, Muvvala S, Carroll KM, Gueorguieva R. An integrated behavioural intervention combined with varenicline for heavy-drinking smokers: a randomized pilot study. J Smok Cessat. 2020 Sep;15(3):119-127. doi: 10.1017/jsc.2020.13. Epub 2020 Mar 18. PMID: 33312238; PMCID: PMC7731353.

8: Hsueh KC, Tang PL, McRobbie H. Effectiveness of Varenicline versus Combination Nicotine Replacement Therapy for Smoking Cessation: One Year Outcomes in a Smoking Cessation Clinic in Taiwan. Nicotine Tob Res. 2021 Feb 4:ntab018. doi: 10.1093/ntr/ntab018. Epub ahead of print. PMID: 33538831.

9: Gray KM, Rubinstein ML, Prochaska JJ, DuBrava SJ, Holstein AR, Samuels L, McRae TD. Effect of varenicline for smoking cessation in adolescents - Authors' reply. Lancet Child Adolesc Health. 2021 Feb;5(2):e4. doi: 10.1016/S2352-4642(20)30395-3. PMID: 33484669.

10: Panda PK, Sharawat IK. Effect of varenicline for smoking cessation in adolescents. Lancet Child Adolesc Health. 2021 Feb;5(2):e3. doi: 10.1016/S2352-4642(20)30396-5. PMID: 33484668.

11: May JR, Jao NC, McCarter K, Klass E, Pearman T, Leone F, Schnoll RA, Hitsman B. Change in Health-Related Quality of Life Among Individuals With Cancer Undergoing Smoking Cessation Treatment Involving Varenicline. Oncol Nurs Forum. 2021 Jan 4;48(1):112-120. doi: 10.1188/21.ONF.112-120. PMID: 33337436; PMCID: PMC7983103.

12: Carpenter MJ, Gray KM, Wahlquist AE, Cropsey K, Saladin ME, Froeliger B, Smith TT, Toll BA, Dahne J. A Pilot Randomized Clinical Trial of Remote Varenicline Sampling to Promote Treatment Engagement and Smoking Cessation. Nicotine Tob Res. 2020 Nov 29:ntaa241. doi: 10.1093/ntr/ntaa241. Epub ahead of print. PMID: 33249458.

13: Lawson SC, Gass JC, Cooper RK Jr, Tonkin SS, Colder CR, Mahoney MC, Tiffany ST, Hawk LW Jr. The impact of three weeks of pre-quit varenicline on reinforcing value and craving for cigarettes in a laboratory choice procedure. Psychopharmacology (Berl). 2021 Feb;238(2):599-609. doi: 10.1007/s00213-020-05713-7. Epub 2020 Nov 21. PMID: 33219852.

14: Alhowail A. Varenicline enhances the survival of doxorubicin-treated mice. Eur Rev Med Pharmacol Sci. 2020 Nov;24(21):11350-11355. doi: 10.26355/eurrev_202011_23626. PMID: 33215455.

15: Thomas KH, Davies NM, Taylor AE, Taylor GMJ, Gunnell D, Martin RM, Douglas I. Risk of neuropsychiatric and cardiovascular adverse events following treatment with varenicline and nicotine replacement therapy in the UK Clinical Practice Research Datalink: a case-cross-over study. Addiction. 2020 Nov 16. doi: 10.1111/add.15338. Epub ahead of print. PMID: 33197082.

16: Madae'en S, Obeidat N, Adeinat M. Using cost-effectiveness analysis to support policy change: varenicline and nicotine replacement therapy for smoking cessation in Jordan. J Pharm Policy Pract. 2020 Oct 27;13:65. doi: 10.1186/s40545-020-00270-y. PMID: 33117544; PMCID: PMC7590594.

17: Thompson BM, Barrett ST, Huynh YW, Kwan DA, Murray JE, Bevins RA. The importance of acquisition learning on nicotine and varenicline drug substitution in a drug-discriminated goal-tracking task. Pharmacol Biochem Behav. 2020 Dec;199:173045. doi: 10.1016/j.pbb.2020.173045. Epub 2020 Oct 12. PMID: 33058788; PMCID: PMC7725853.

18: Gobarani RK, Abramson MJ, Bonevski B, Weeks GR, Dooley MJ, Smith BJ, Veale A, Webb A, Kirsa S, Thomas D, Miller A, Gasser R, Paul E, Parkinson J, Meanger D, Coward L, Kopsaftis Z, Rofe O, Lee P, George J. The efficacy and safety of varenicline alone versus in combination with nicotine lozenges for smoking cessation among hospitalised smokers (VANISH): study protocol for a randomised, placebo-controlled trial. BMJ Open. 2020 Oct 6;10(10):e038184. doi: 10.1136/bmjopen-2020-038184. PMID: 33028555; PMCID: PMC7539569.

19: Morphett K, Connor JP. Varenicline for smoking cessation in young people: is there more we need to know? Lancet Child Adolesc Health. 2020 Nov;4(11):797-799. doi: 10.1016/S2352-4642(20)30305-9. Epub 2020 Sep 25. PMID: 32979940.

20: Gray KM, Rubinstein ML, Prochaska JJ, DuBrava SJ, Holstein AR, Samuels L, McRae TD. High-dose and low-dose varenicline for smoking cessation in adolescents: a randomised, placebo-controlled trial. Lancet Child Adolesc Health. 2020 Nov;4(11):837-845. doi: 10.1016/S2352-4642(20)30243-1. Epub 2020 Sep 25. PMID: 32979939.