U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 41 - 50 of 186 results

Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)



N-(4-(2-Methoxyphenoxy)-phenyl-N-(2,2,2-trifluoroethylsulfonyl)-pyrid-3-ylmethylamine (LY487379) is a selective positive allosteric modulator at metabotropic glutamate subtype 2 receptors (mGluR2). The compound exerts antipsychotic and anxiolytic actions.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

CBiPES is a selective positive allosteric modulator of the metabotropic glutamate receptor group II subtype mGluR2. CBiPES attenuated a stress-induced hyperthermia and PCP-induced hyperlocomotor activity in the mouse model.
U 89843A is a positive allosteric modulator of GABAA receptors. U 89843A enhances GABA-induced Cl- currents in the α1β2γ2, α3β2γ2 and α6β2γ2 subtypes. Causes sedation in vivo following i.v. administration without losing "righting reflex". U 89843A has sedative effects in animals but without causing ataxia, and also acts as an antioxidant and may have neuroprotective effects.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Ro 67-4853 exhibited activity at all group I of metabotropic glutamate receptors including mGluR1 and mGluR5. It enhances the effects of (S)-DHPG in CA3 neurons. Site-directed mutagenesis revealed that valine at position 757 in transmembrane V of mGluR1 is crucial for the activity of multiple classes of allosteric mGluR1 potentiators. The discovery of selective mGluR1 enhancers opens the possibility for therapeutically relevant positive modulation of family 3 G proteincoupled receptors.