Velnacrine

Last updated
Velnacrine
Velnacrine.svg
Names
IUPAC name
9-amino-1,2,3,4-tetrahydroacridin-1-ol
Identifiers
3D model (JSmol)
PubChem CID
  • InChI=1S/C13H14N2O/c14-13-8-4-1-2-5-9(8)15-10-6-3-7-11(16)12(10)13/h1-2,4-5,11,16H,3,6-7H2,(H2,14,15)
  • C1CC(C2=C(C3=CC=CC=C3N=C2C1)N)O
Properties
C13H14N2O
Molar mass 214.268 g·mol−1
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).

Velnacrine, also known as 1-hydroxytacrine [1] , is an inhibitor of cholinesterase enzymes. It is also a metabolite of tacrine. [2]

Contents

Pharmacology

Velnacrine is able to inhibit acetylcholinesterase (AChE) [3] , this results in elevated levels of acetylcholine, as AChE is the enzyme that hydrolyzes acetylcholine. [4] It is also able to inhibit butyrylcholinesterase. [5]

Therapeutic potential

Velnacrine, as many other cholinergics, has been described as possibly useful to help manage symptoms of Alzheimer's disease. Some research has described the drug as having benefits over placebo [6] and an acceptable safety profile. [7] However, a review described available data as not proving efficacy and showing evidence of toxicity. [8] Additionally, the FDA voted against recommending approval of velnacrine. [8]

References

  1. ↑ PubChem. "Velnacrine". pubchem.ncbi.nlm.nih.gov. Retrieved 2025-07-31.
  2. ↑ Viau, C. J.; Curren, R. D.; Wallace, K. (1993). "Cytotoxicity of tacrine and velnacrine metabolites in cultured rat, dog and human hepatocytes". Drug and Chemical Toxicology. 16 (3): 227–239. doi:10.3109/01480549309081817. ISSN   0148-0545. PMID   8404544.
  3. ↑ "AID 31170 - Inhibition of acetylcholinesterase (AChE) of human red blood cell (type XIII) by modified radiometric AChE assay - PubChem". pubchem.ncbi.nlm.nih.gov. Retrieved 2025-07-31.
  4. ↑ Trang, Amy; Khandhar, Paras B. (2025), "Physiology, Acetylcholinesterase", StatPearls, Treasure Island (FL): StatPearls Publishing, PMID   30969557 , retrieved 2025-07-31
  5. ↑ "AID 44453 - Inhibition of (BChE) Butyrylcholinesterase of horse serum - PubChem". pubchem.ncbi.nlm.nih.gov. Retrieved 2025-07-31.
  6. ↑ Antuono, P. G. (1995-09-11). "Effectiveness and safety of velnacrine for the treatment of Alzheimer's disease. A double-blind, placebo-controlled study. Mentane Study Group". Archives of Internal Medicine. 155 (16): 1766–1772. doi:10.1001/archinte.1995.00430160102010. ISSN   0003-9926. PMID   7654110.
  7. ↑ Puri, S. K.; Ho, I.; Hsu, R.; Lassman, H. B. (October 1990). "Multiple dose pharmacokinetics, safety, and tolerance of velnacrine (HP 029) in healthy elderly subjects: a potential therapeutic agent for Alzheimer's disease". Journal of Clinical Pharmacology. 30 (10): 948–955. doi:10.1002/j.1552-4604.1990.tb03576.x. ISSN   0091-2700. PMID   2229455.
  8. 1 2 Birks, J.; Wilcock, G. G. W. (2004). "Velnacrine for Alzheimer's disease". The Cochrane Database of Systematic Reviews (2): CD004748. doi:10.1002/14651858.CD004748. ISSN   1469-493X. PMID   15106259.
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