Potent and selective agonist of the delta opioid receptor
AZD2327
Names
IUPAC name
4-[(R)-(3-aminophenyl)-[4-[(4-fluorophenyl)methyl]piperazin-1-yl]methyl]-N,N-diethylbenzamide
Identifiers
ECHA InfoCard
100.170.827
Properties
C 29 H 35 F N 4 O
Molar mass
474.624 g·mol−1
Except where otherwise noted, data are given for materials in their
standard state (at 25 °C [77 °F], 100 kPa).
Chemical compound
AZD2327 is a drug used in scientific research, it is being investigated for the treatment of anxiety.
AZD2327 appears to be a selective and strong agonist of the delta opioid receptor , it is also an inhibitor of CYP3A4.[ 1]
In a study, AZD2327 has been shown to inhibit the release of noradrenaline caused by anxiety, it was able to inhibit it as much as diazepam .[ 2] However, in this case, AZD2327 could be a better option than diazepam, because benzodiazepines (such as diazepam) often cause rapid tolerance and physical dependence,[ 3] however, it seems like AZD2327 does not cause tolerance development.[ 2]
Another study has also concluded by mentioning that AZD2327 has potential as an anxiolytic.[ 4]
It is also worth noting that AZD2327 appears to have a low potential of abuse,[ 5] unlike certain anxiolytics such as benzodiazepines which are easily abusable.
^ Guo, Jian; Zhou, Diansong; Li, Yan; Khanh, Bui H. (November 2015). "Physiologically based pharmacokinetic modeling to predict complex drug–drug interactions: a case study of AZD2327 and its metabolite, competitive and time-dependent CYP3A inhibitors" . Biopharmaceutics & Drug Disposition . 36 (8): 507–519. doi :10.1002/bdd.1962 . ISSN 0142-2782 . PMID 26081137 .
^ a b Hudzik, T. J.; Maciag, C.; Smith, M. A.; Caccese, R.; Pietras, M. R.; Bui, K. H.; Coupal, M.; Adam, L.; Payza, K.; Griffin, A.; Smagin, G.; Song, D.; Swedberg, M. D. B.; Brown, W. (July 2011). "Preclinical pharmacology of AZD2327: a highly selective agonist of the δ-opioid receptor" . The Journal of Pharmacology and Experimental Therapeutics . 338 (1): 195–204. doi :10.1124/jpet.111.179432 . ISSN 1521-0103 . PMID 21444630 .
^ Rosenberg, Howard C.; Chiu, Ted H. (March 1985). "Time course for development of benzodiazepine tolerance and physical dependence" . Neuroscience & Biobehavioral Reviews . 9 (1): 123–131. doi :10.1016/0149-7634(85)90038-7 . PMID 2858077 .
^ Richards, Erica M.; Mathews, Daniel C.; Luckenbaugh, David A.; Ionescu, Dawn F.; Machado-Vieira, Rodrigo; Niciu, Mark J.; Duncan, Wallace C.; Nolan, Neal M.; Franco-Chaves, Jose A.; Hudzik, Thomas; Maciag, Carla; Li, Shuang; Cross, Alan; Smith, Mark A.; Zarate, Carlos A. (March 2016). "A randomized, placebo-controlled pilot trial of the delta opioid receptor agonist AZD2327 in anxious depression" . Psychopharmacology . 233 (6): 1119–1130. doi :10.1007/s00213-015-4195-4 . ISSN 0033-3158 . PMC 5103283 . PMID 26728893 .
^ Hudzik, T.J.; Pietras, M.R.; Caccese, R.; Bui, K.H.; Yocca, F.; Paronis, C.A.; M.D.B., Swedberg (September 2014). "Effects of the δ opioid agonist AZD2327 upon operant behaviors and assessment of its potential for abuse" . Pharmacology Biochemistry and Behavior . 124 : 48–57. doi :10.1016/j.pbb.2014.05.009 . PMID 24857840 .