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RES-701-1, a novel, potent, endothelin type B receptor-selective antagonist of microbial origin.
The results suggest that RES-701-1 is a potent and specific antagonist for the ETB receptor and that it will be a powerful tool for understanding the physiological roles of this receptor.
The role of adenosine A2a receptors in regulating GABAergic synaptic transmission in striatal medium spiny neurons.
- A. Mori, T. Shindou, M. Ichimura, H. Nonaka, H. Kase
- Biology, MedicineThe Journal of neuroscience : the official…
- 15 January 1996
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
KF17837 ((E)-8-(3,4-dimethoxystyryl)-1,3-dipropyl-7-methylxanthine), a potent and selective adenosine A2 receptor antagonist.
Unique binding pocket for KW-4679 in the histamine H1 receptor.
8-Polycycloalkyl-1,3-dipropylxanthines as potent and selective antagonists for A1-adenosine receptors.
- J. Shimada, F. Suzuki, H. Nonaka, A. Ishii
- Chemistry, MedicineJournal of medicinal chemistry
- 6 March 1992
1,3-Dipropyl-8-(3-noradamantyl)xanthine was identified to be a selective and the most potent A1 receptor antagonist reported to date and under the structure-activity relationship, the 8-substituent of xanthine antagonists and the N6- substituents of adenosine agonists appears to bind to the same region of the A1 receptors.
Carbon-11-labeled KF21213: a highly selective ligand for mapping CNS adenosine A(2A) receptors with positron emission tomography.
Binding of [3H]KF17837S, a selective adenosine A2 receptor antagonist, to rat brain membranes.
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.