Ro 41-1049
Ro 41-1049 is a highly selective, reversible MAO-A inhibitor. Ro 41-1049 effectively blocks the Quinpirole (HY-B1752)-induced increase in dopamine D2-like receptor density in the nucleus accumbens and alters the pattern of behavioral sensitization, shifting animals' responses from enhanced motor activity to immobile self-directed gaping behavior. Tritium-labeled Ro 41-1049 serves as a high-affinity radioligand, enabling accurate mapping of the distribution and abundance of MAO-A in the central nervous system, peripheral organs, and human brain via quantitative enzyme autoradiography. Ro 41-1049 can be used for basic research on depression and other related diseases.
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- No. CAS: 127500-84-9
- Fòrmula: C12H12FN3OS
- Peso molecular:265.31
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
D2 Receptor |
MAO-A |
In Vitro
Ro 41-1049 (10 μM; 4 hrs) inhibits a portion of in vitro [3H]quinpirole binding to dopamine D2-like receptors in nucleus accumbens and striatum tissue homogenates, though this inhibitory effect is not modulated by prior in vivo quinpirole or Ro 41-1049 treatments[1].
Tritiated Ro 41-1049 (1-150 nM; 60 min) binds to MAO-A in rat cerebral cortex sections with high affinity (Kd = 10.7 nM) and a maximum binding capacity of 7.38 pmol/mg protein, with consistent high-affinity binding across rat brain regions[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Long-Evans (male, 200-230 g at study start)[1]
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Dosage:1 mg/kg
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Administration:s.c.; 90 minutes prior to each quinpirole injection; twice weekly for 8 pairs of injections
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Result:Increased total mouthing after the 8th injection to 7-times higher than in saline control rats.
Reduced [3H]spiperone binding in the nucleus accumbens by 38% compared to quinpirole-sensitized rats without Ro 41-1049 pre-treatment.
Prevented the 32% increase in [3H]quinpirole and [3H]spiperone binding observed in the nucleus accumbens of quinpirole-sensitized rats, with receptor binding levels matching saline controls.
Showed no alterations in dopamine D2-like receptor binding, percentage of receptors in the high affinity state, or percentage of MAO inhibitor-inhibitable [3H]quinpirole binding in the striatum.
Resulted in distance traveled not different from saline controls.
Chemical Information
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No. CAS 127500-84-9
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Peso molecular 265.31
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Fòrmula C12H12FN3OS
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SMILES
O=C(NCCN)C=1N=CSC1C=2C=CC=C(F)C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Ro 41-1049 Related Classifications
HY-100027 Related Classifications
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