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Pharmacology of the octopamine receptor from locust central nervous tissue (OAR3)
Author(s) -
Roeder Thomas
Publication year - 1995
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1995.tb14927.x
Subject(s) - locust , octopamine (neurotransmitter) , receptor , stereochemistry , biology , migratory locust , biochemistry , chemistry , serotonin , botany
1 The present study characterized highly effective agonists from different classes of compounds for the neuronal octopamine receptor (OAR 3 ) of the migratory locust ( Locusta migratoria L.). Biogenic amines and phenyliminoimidazolidines (PIIs) were employed for the study of structure‐activity relationships. 2 The highest affinity PIIs were predominantly those with substitutions at the positions 2 and 4 of the phenolic ring (e.g. NC 7, K I = 0.3 n m , NC 8, K I = 0.81 n m ). Substitutions at these positions always had positive effects on the affinity of the respective agonists. 3 Substitutions at the positions 3, 5 and 6, however, always had negative effects on the affinity. At the position one of the phenolic ring, heterocyclic substituents are preferred. 4 Some PIIs had a more than 30 times higher affinity for OARs than for α‐adrenoceptors which are the vertebrate homologues of the insect octopamine receptors. 5 The only non‐PII with subnanomolar affinity was the aminooxazoline derivative AC 6 ( K I = 0.92 n m ). 6 A variety of substances with known insecticidal activity such as chlordimeform, demethylchlor‐dimeform, amitraz or AC 6 had high affinity for the locust neuronal octopamine receptor.