(R)-(-)-Apomorphine hydrochloride - CAS 314-19-2
Category: Inhibitor
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Dopamine Receptor
(R)-(-)-Apomorphine hydrochloride is the hydrochloride salt of apomorphine, which is a prototypical non-selective dopamine D2 agonist. It exhibits pKi values of 6.43, 7.08, 7.59, 8.36, and 7.83 for human recombinant D1, D2L, D3, D4, and D5 receptors, respectively. It produces biphasic effects on locomotor activity and shows neuroprotective actions following systemic administration in vivo. It has the potential for the treatment of Parkinson's disease. It also promotes intraneuronal amyloid-β (Aβ) degradation and improves memory function in an Alzheimer's disease model. It may improve brain insulin resistance.
≥99% by HPLC
5,6,6aR,7-tetrahydro-6-methyl-4H-dibenzo[de,g]quinoline-10,11-diol, monohydrochloride; (6aR)-5,6,6a,7-Tetrahydro-6-methyl-4H-dibenzo[de,g]quinoline-10,11-diol Hydrochloride; (R)-5,6,6a,7-Tetrahydro-6-methyl-4H-dibenzo[de,g]quinoline-10,11-diol Hydrochloride; 6aβ-Aporphine-10,11-diol Hydrochloride; (-)-Apomorphine Hydrochloride; Apomorphine Hydrochloride; Uprima
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1.Electrophysiological and behavioral assessments of dopamine autoreceptor activation to apomorphine in rats.
Okuyama S;Shimamura H;Hashimoto S;Aihara H Arch Int Pharmacodyn Ther. 1986 Dec;284(2):246-54.
Single neuronal activity was recorded extracellularly in the substantia nigra pars compacta (SNC) in rats anesthetized with chloral hydrate. Haloperidol in a dose of 10 micrograms/kg had no significant effects on the SNC neurons. R(-)apomorphine (cumulative i.v. dose of 40 micrograms/kg, given as: 5, 5, 10 and 20 micrograms/kg) inhibited the firing rate of dopaminergic neurons, in a dose-dependent manner. Haloperidol (cumulative i.v. dose of 10 micrograms/kg, as: 2.5, 2.5 and 5 micrograms/kg) reversed the effect of apomorphine. Complete reversal of the firing rate to haloperidol was observed with a dose of 10 micrograms/kg. In rats pretreated with 10 micrograms/kg of haloperidol, there was a dramatic shift to the right of the apomorphine dose-response curve (cumulative i.v. dose of 800 micrograms/kg, as: 50, 50, 100, 200 and 400 micrograms/kg), and this inhibition was reversed by haloperidol (cumulative i.v. dose of 400 micrograms/kg, as: 50, 50, 100 and 200 micrograms/kg). Apomorphine in doses of 40 micrograms/kg and 800 micrograms/kg elicited yawning behavior and stereotypy, respectively. Apomorphine in a dose of 800 micrograms/kg elicited stereotypy in rats treated 3 min before with 10 micrograms/kg of haloperidol.
2.Reinforcing effects of D2 dopamine receptor agonists and partial agonists in rhesus monkeys.
Ranaldi R;Wang Z;Woolverton WL Drug Alcohol Depend. 2001 Oct 1;64(2):209-17.
Dopamine (DA) receptors play a role in the reinforcing effects of psychomotor stimulants and other drugs. Both D1 and D2 DA receptor agonists have been reported to function as positive reinforcers in maintaining self-administration in non-human subjects. The purpose of the present study was to evaluate, in monkeys, the reinforcing effects of DA D2 receptor agonists that vary in their efficacy as D2 agonists. Rhesus monkeys were prepared with venous catheters and lever pressing was maintained by i.v. cocaine (n=5, 0.03 mg/kg/inj) in daily baseline sessions (2 h/day, fixed ratio 25). Various doses of cocaine or D2 agonists were then made available for at least four to seven sessions, and until responding was stable. At least one dose of the higher-efficacy D2 agonists, R(-)-propylnorapomorphine (NPA) (n=4, 0.001-0.01 mg/kg/inj), R(-)-apomorphine (APO) (n=4, 0.003-0.1 mg/kg/inj) and R(+)-3-(3-hydroxyphenyl)-N-propylpiperidine HCl [R(+)-3-PPP] (n=4, 0.03-0.3 mg/kg/inj), functioned as a positive reinforcer in all the monkeys tested. In contrast, no dose of the lower-efficacy D2 agonists, R(+)-terguride (n=4, 0.001-0.3 mg/kg/inj) and S(-)-3-(3-hydroxyphenyl)-N-propylpiperidine HCl [S(-)-3-PPP] (n=4, 0.
3.Proton-coupled organic cation antiporter-mediated uptake of apomorphine enantiomers in human brain capillary endothelial cell line hCMEC/D3.
Okura T;Higuchi K;Kitamura A;Deguchi Y Biol Pharm Bull. 2014;37(2):286-91. Epub 2013 Nov 20.
R(-)-Apomorphine is a dopamine agonist used for rescue management of motor function impairment associated with levodopa therapy in Parkinson's disease patients. The aim of this study was to examine the role of proton-coupled organic cation antiporter in uptake of R(-)-apomorphine and its S-enantiomer in human brain, using human endothelial cell line hCMEC/D3 as a model. Uptake of R(-)- or S(+)-apomorphine into hCMEC/D3 cells was measured under various conditions to evaluate its time-, concentration-, energy- and ion-dependency. Inhibition by selected organic cations was also examined. Uptakes of both R(-)- and S(+)-apomorphine increased with time. The initial uptake velocities of R(-)- and S(+)-apomorphine were concentration-dependent, with similar Km and Vmax values. The cell-to-medium (C/M) ratio of R(-)-apomorphine was significantly reduced by pretreatment with sodium azide, but was not affected by replacement of extracellular sodium ion with N-methylglucamine or potassium. Intracellular alkalization markedly reduced the uptake, while intracellular acidification increased it, suggesting that the uptake is driven by an oppositely directed proton gradient. The C/M ratio was significantly decreased by amantadine, verapamil, pyrilamine and diphenhydramine (substrates or inhibitors of proton-coupled organic cation antiporter), while tetraethylammonium (substrate of organic cation transporters (OCTs)) and carnitine (substrate of carnitine/organic cation transporter 2; (OCTN2)) had no effect.
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CAS 314-19-2 (R)-(-)-Apomorphine hydrochloride

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