Orru, Marco published the artcileStriatal pre- and postsynaptic profile of adenosine A2A receptor antagonists, SDS of cas: 377727-87-2, the publication is PLoS One (2011), 6(1), e16088, database is CAplus and MEDLINE.
Striatal adenosine A2A receptors (A2ARs) are highly expressed in medium spiny neurons (MSNs) of the indirect efferent pathway, where they heteromerize with dopamine D2 receptors (D2Rs). A2ARs are also localized presynaptically in cortico-striatal glutamatergic terminals contacting MSNs of the direct efferent pathway, where they heteromerize with adenosine A1 receptors (A1Rs). It was hypothesized that postsynaptic A2AR antagonists should be useful in Parkinson’s disease, while presynaptic A2AR antagonists could be beneficial in dyskinetic disorders, such as Huntington’s disease, obsessive-compulsive disorders and drug addiction. The aim or this work was to determine whether selective A2AR antagonists may be subdivided according to a preferential pre- vs. postsynaptic mechanism of action. The potency at blocking the motor output and striatal glutamate release induced by cortical elec. stimulation and the potency at inducing locomotor activation were used as in vivo measures of pre- and postsynaptic activities, resp. SCH-442416 and KW-6002 showed a significant preferential pre- and postsynaptic profile, resp., while the other tested compounds (MSX-2, SCH-420814, ZM-241385 and SCH-58261) showed no clear preference. Radioligand-binding experiments were performed in cells expressing A2AR-D2R and A1R-A2AR heteromers to determine possible differences in the affinity of these compounds for different A2AR heteromers. Heteromerization played a key role in the presynaptic profile of SCH-442416, since it bound with much less affinity to A2AR when co-expressed with D2R than with A1R. KW-6002 showed the best relative affinity for A2AR co-expressed with D2R than co-expressed with A1R, which can at least partially explain the postsynaptic profile of this compound Also, the in vitro pharmacol. profile of MSX-2, SCH-420814, ZM-241385, and SCH-58261 was is in accordance with their mixed pre- and postsynaptic profile. On the basis of their preferential pre- vs. postsynaptic actions, SCH-442416 and KW-6002 may be used as lead compounds to obtain more effective antidyskinetic and antiparkinsonian compounds, resp.
PLoS One published new progress about 377727-87-2. 377727-87-2 belongs to triazoles, auxiliary class GPCR/G Protein,Adenosine Receptor, name is 2-(Furan-2-yl)-7-(2-(4-(4-(2-methoxyethoxy)phenyl)piperazin-1-yl)ethyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine, and the molecular formula is C25H29N9O3, SDS of cas: 377727-87-2.
Referemce:
https://en.wikipedia.org/wiki/1,2,3-Triazole,
Triazoles – an overview | ScienceDirect Topics