The property profile of N-decyltropine (IEM-1556) has significant advantages over that of its prototype, the selective nicotinic receptor antagonist tert-butyldecylammonium (IEM-1678), because its anticonvulsant, antiparkinsonian, antidepressant, and analgesic activities are significantly greater and its therapeutic index is 2.8 times higher than that of IEM-1678. The higher pharmacological activity and lower toxicity of IEM-1556 are explained by the fact that IEM-1556 not only blocks nicotinic receptors but also stimulates subdiaphragmatic vagal afferents.
Similar content being viewed by others
References
I. N. Remizov, V. Y. Maslov, E. E. Purnyn, et al., Neurophysiology, 27(5 – 6), 255 – 260 (1995).
A. Tsybenko, P. I. Yanchuk, L. S. Egorova, and V. E. Gmiro, Neurophysiology, 28(2/3), 119 – 125 (1996).
V. E. Gmiro and S. E. Serdyuk, Ross. Zh. Fiziol. im. I. M. Sechenova, 103(10), 1106 – 1113 (2017).
V. E. Gmiro and S. E. Serdyuk, J. Pharm. Drug Delivery Res., 5, Issue 4 (Suppl.), 81 (2016).
V. E. Gmiro, L. K. Gavrovskaya, E. N. Kharchevnikova, et al., RU Pat. No. 2,014,074, Jun. 15, 1994; Byull. Izobret., No. 11 (1994).
S. E. Serdyuk and V. E. Gmiro, Byull. Eksp. Biol. Med., 143(5), 548 – 550 (2007).
S. E. Serdyuk and V. E. Gmiro, Eksp. Klin. Farmakol., 71(4), 14 – 17 (2008).
S. E. Krahl, S. S. Senanayake, and A. Handforth, Epilepsy Res., 38(2 – 3), 171 – 175 (2000).
V. E. Gmiro and S. E. Serdyuk, Byull. Eksp. Biol. Med., 143(5), 554 – 556 (2007).
S. E. Serdyuk and V. E. Gmiro, Byull. Eksp. Biol. Med., 144(11), 535 – 537 (2007).
R. D. Porsolt, G. Anton, N. Blavet, and M. Jalfre, Eur. J. Pharmacol., 47(4), 379 – 391 (1978).
Author information
Authors and Affiliations
Corresponding author
Additional information
Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 53, No. 3, pp. 21 – 25, March, 2019.
Rights and permissions
About this article
Cite this article
Gmiro, V.E., Serdyuk, S.E. Synthesis and Pharmacological Properties of N-Decyltropine (IEM-1556) as Compared to Selective Nicotinic Receptor Antagonist Tert-Butyldecylammonium (IEM-1678). Pharm Chem J 53, 212–215 (2019). https://doi.org/10.1007/s11094-019-01981-6
Received:
Published:
Issue Date:
DOI: https://doi.org/10.1007/s11094-019-01981-6