Antagonism of the effects of (+)-PD 128907 on midbrain dopamine neurones in rat brain slices by a selective D2 receptor antagonist L-741,626

British Journal of Pharmacology
B BoweryG R Seabrook

Abstract

1. The ability of PD 128907 to activate dopamine receptors in the ventral tegmental area, substantia nigra pars compacta, and striatum was investigated by use of in vitro electrophysiological recording and fast cyclic voltammetry. The affinity of a novel D2 selective antagonist L-741,626 for receptors activated by this agonist was measured to determine if its effects were mediated by D2 or D3 receptors. 2. The active (+) enantiomer of PD 128907 bound with high affinity and selectivity to rat D3 dopamine receptors. The Ki values for (+)-PD 128907 were 620 nM at D2, 1 nM at D3 and 720 nM at D4 receptors. 3. (+)-PD 128907 inhibited cell firing in both the ventral tegmental area and substantia nigra pars compacta with EC50 values of 33 nM (pEC50 = 7.48 +/- 0.10, n = 10) and 38 nM (pEC50 = 7.42 +/- 0.15, n = 5), respectively. No effects of (+)-PD 128907 (100 nM) were observed on glutamate or GABA-mediated synaptic potentials elicited by focal bipolar stimulation. 4. L-741,626 antagonized these effects of (+)-PD 128907 in a concentration-dependent and surmountable manner with an affinity, determined from Schild analysis, of 20 nM (pKB = 7.71 +/- 0.14) in the ventral tegmental area and 11 nM (pKB = 7.95 +/- 0.18) in the substantia nig...Continue Reading

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Citations

Dec 13, 2000·Pharmacology, Biochemistry, and Behavior·J J Canales, S D Iversen
Dec 5, 1998·Pharmacology & Therapeutics·P A JoseR A Felder
Aug 4, 2012·The Journal of Pharmacology and Experimental Therapeutics·Stephanie M Perez, Daniel J Lodge
May 4, 2012·Journal of Neurophysiology·Andrew M DacksAlan J Nighorn
Oct 2, 2009·International Journal of Cancer. Journal International Du Cancer·Monique CoufalSharon DeMorrow
Feb 7, 2006·Neuropharmacology·Richard G HunterMichael J Kuhar
Oct 26, 2013·Neuropharmacology·Celina Y MojicaFrances M Leslie
Oct 27, 2009·Behavioural Brain Research·Panayotis K ThanosNora D Volkow
Oct 6, 2010·Journal of Pharmacological Sciences·Saori ShimadaYoshihisa Ito
Dec 1, 2006·The Journal of Pharmacology and Experimental Therapeutics·Anton BespalovGerhard Gross
Aug 21, 2020·Pflügers Archiv : European journal of physiology·José Ángel García-PedrazaMónica García-Domingo
Feb 7, 2021·Molecular Cell·Peiyu XuH Eric Xu

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