Behavioral and radioligand binding evidence for irreversible dopamine receptor blockade by N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline
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Cited by (128)
Importance of D1 and D2 receptor stimulation for the induction and expression of cocaine-induced behavioral sensitization in preweanling rats
2017, Behavioural Brain ResearchCitation Excerpt :These experiments employed a one-trial sensitization procedure in order to minimize the effects of tolerance and dependence, while permitting an unbiased measure of induction and expression [33]. In separate experiments, the irreversible receptor antagonist N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ), which has a high affinity for D1 and D2, 5-HT1A and 5-HT2A, α2-adrenergic, and GABAA receptors [36–42], was administered 24 h before the induction or expression of behavioral sensitization. To determine the relative involvement of DA receptors in these processes, selective DA antagonists were used to protect D1 and/or D2 receptors from EEDQ-induced receptor alkylation [43–46].
Potent haloperidol derivatives covalently binding to the dopamine D2 receptor
2017, Bioorganic and Medicinal ChemistryCitation Excerpt :Due to the current absence of crystal structures of an antagonist-bound dopamine D2 receptor, substantial efforts have to be invested to learn more about the receptor-ligand interactions responsible for the stabilization of the receptor in its inactive state. To our knowledge, only a few covalent ligands have been reported to irreversibly antagonize the D2-receptors.30–32 In this work, we synthesized a set of covalent ligands derived from the classical antipsychotic drug haloperidol and the covalent dopamine analog FAUC150 irreversibly binding to a L94C cysteine mutant of the dopamine D2 receptor.7
Dopamine receptor inactivation in the caudate-putamen differentially affects the behavior of preweanling and adult rats
2012, NeuroscienceCitation Excerpt :The reason for this age-dependent difference has not been determined. In adult rats, EEDQ has been microinjected into various brain regions in order to examine whether D1 and/or D2 receptor stimulation contributes to the mediation of muscle tone, various unlearned behaviors, ipsilateral circling, and fixed-interval operant responding (Hamblin and Creese, 1983; Bordi et al., 1989; Cameron and Crocker, 1989; Giorgi and Biggio, 1990a,b; Lee et al., 1995; Neisewander et al., 1995; Hemsley et al., 2002; Cory-Slechta et al., 2002). For example, Neisewander et al. (1995) have shown that infusing EEDQ into the lateral CPu attenuates the SKF38393-induced grooming and oral movements of adult rats.
Biogenic amines in the nervous system of the cockroach, Periplaneta americana following envenomation by the jewel wasp, Ampulex compressa
2012, ToxiconCitation Excerpt :It is therefore possible that Ampulex venom somehow interferes either with dopamine receptor function or the downstream signaling cascade resulting from receptor activation. Although there is scant information regarding dopamine receptor turnover in insects, it has been demonstrated previously that dopamine receptor turnover in rats takes around 7–10 days (Hamblin and Creese, 1983), similar to the time course of recovery from hypokinesia. These data suggest that even though dopamine levels are unchanged in stung animals, dopaminergic signaling overall may be compromised.
Alkylation of rat dopamine transporters and blockade of dopamine uptake by EEDQ
2000, Neuropharmacology