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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.
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.
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.
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.
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.