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Etoperidone
Introduction
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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