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The role of adenosine A2a receptors in regulating GABAergic synaptic transmission in striatal medium spiny neurons.
TLDR
The A2a receptor may regulate striatal output activity by relieving GABA-mediated inhibition of the medium spiny projection neurons, which explains the ability of purinergic agents to affect motor control.
Adenosine A2A antagonists with potent anti-cataleptic activity
Abstract Structure-activity relationship of 8-styrylxanthines for in vivo adenosine A2A antagonism were explored. Diethyl substitution both at the 1- and 3-position was found to dramatically
KF17837 ((E)-8-(3,4-dimethoxystyryl)-1,3-dipropyl-7-methylxanthine), a potent and selective adenosine A2 receptor antagonist.
TLDR
The results indicate that KF17837S (and hence KF 17837) is a highly potent and selective adenosine A2A receptor antagonist.
Unique binding pocket for KW-4679 in the histamine H1 receptor.
TLDR
It is demonstrated that the tested tri- and tetracyclic histamine H1 receptor antagonists which have a tight interaction with the Asp residue are not selective for the histamineH1 receptor.
Binding of [3H]KF17837S, a selective adenosine A2 receptor antagonist, to rat brain membranes.
TLDR
Data indicate that [3H] KF17837S labels the adenosine A2A receptor in rat brain, and a strong positive correlation was observed between the pharmacological profiles for these two radioligand assays.
Correlation between emetic effect of phosphodiesterase 4 inhibitors and their occupation of the high-affinity rolipram binding site in Suncus murinus brain.
TLDR
It is concluded that the emetic effect of phosphodiesterase 4 inhibitors is caused at least in part via binding to the high-affinity rolipram binding site in brain in vivo.
Duocarmycin SA, a new antitumor antibiotic from Streptomyces sp.
Adenosine A2A receptor enhances GABAA‐mediated IPSCs in the rat globus pallidus
TLDR
The results suggest that A2A receptors in the GP serve to inhibit GP neuronal activity, thereby disinhibiting subthalamic nucleus neurone activity, and may play a crucial role in controlling the neuronal functions of basal ganglia.
Presynaptic adenosine A2A receptors enhance GABAergic synaptic transmission via a cyclic AMP dependent mechanism in the rat globus pallidus
TLDR
The results indicate that A2A receptor‐mediated potentiation of mIPSCs in the GP involves the sequential activation of the A 2A receptor, adenylyl cyclase, and then PKA, and that this facilitatory modulation could occur independently of presynaptic Ca2+ influx.
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