Etoperidone
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]
Overview
Overview
Etoperidone (Axiomin, Centren, Depracer, Etonin, Etoran, Staff, Tropene), also known as clopradone and triazolinone, is an antidepressant of the phenylpiperazine class which was introduced in Europe in 1977.[1][2] It acts primarily as an antagonist of several receptors in the following order of potency: 5-HT2A receptor (36 nM) > α1-adrenergic receptor (38 nM) > 5-HT1A receptor (85 nM) > α2-adrenergic receptor (570 nM);[3] it has only very weak or negligible affinity for blocking the following receptors: D2 receptor (2,300 nM) > H1 receptor (3,100 nM) > mACh receptors (>35,000 nM).[3] In addition to its receptor blockade, etoperidone also has weak affinity for the monoamine transporters as well: serotonin transporter (890 nM) > norepinephrine transporter (20,000 nM) > dopamine transporter (52,000 nM).[4]
References
References
- ↑ C. R Ganellin; D. J Triggle; F.. Macdonald (1997). Dictionary of pharmacological agents. CRC Press. p. 859. ISBN 978-0-412-46630-4. Retrieved 27 November 2011.
- ↑ Index nominum 2000: international drug directory. Taylor & Francis US. 2000. p. 421. ISBN 978-3-88763-075-1. Retrieved 27 November 2011.
- ↑ 3.0 3.1 Cusack B, Nelson A, Richelson E. (19941). “Binding of Antidepressants to Human Brain Receptors: Focus on Newer Generation Compounds”. Psychopharmacology (Berl). 114 (4): 559–565. doi:10.1007/BF02244985. PMID 7855217. Check date values in:
|year=(help) - ↑ Tatsumi M, Groshan K, Blakely RD, Richelson E. (1997). “Pharmacological Profile of Antidepressants and Related Compounds at Human Monoamine Transporters”. Eur J Pharmacol. 340 (2–3): 249–258. doi:10.1016/S0014-2999(97)01393-9. PMID 9537821.
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