Abstract:
:Acute dystonic reactions are motor side effects that occur soon after the initiation of neuroleptic treatment. Although earlier studies indicate that these abnormal movements can be induced in animals and humans via activation of sigma receptors, the relative contribution of the different sigma receptor subtypes is unknown. Since sigma(1) and sigma(2) receptor are differentially represented in motor regions of the brain, the affinities of 17 neuroleptics for these sigma receptor subtypes were determined using competition binding studies. The results revealed that most neuroleptics do not exhibit selectivity for either of the sigma receptor subtypes, as reflected by a significant correlation between the affinities of the neuroleptics for sigma(1) vs. sigma(2) receptors. Moreover, when the sigma binding affinities of the neuroleptics were correlated with the tendency of the drugs to produce acute dystonic reactions in humans, there was a significant correlation for both subtypes. Together with earlier studies in animals, the data suggest that neuroleptic-induced motor side effects can be mediated through both sigma(1) and sigma(2) receptors.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Matsumoto RR,Pouw Bdoi
10.1016/s0014-2999(00)00430-1keywords:
subject
Has Abstractpub_date
2000-08-04 00:00:00pages
155-60issue
2eissn
0014-2999issn
1879-0712pii
S0014-2999(00)00430-1journal_volume
401pub_type
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