1. Neuronal Signaling GPCR/G Protein
  2. Monoamine Oxidase Dopamine Receptor
  3. 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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Ro 41-1049

Ro 41-1049 Chemical Structure

CAS No. : 127500-84-9

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Description

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[1][2][3].

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

Pre-treatment with Ro 41-1049 (1 mg/kg; s.c.; 90 minutes prior to each Quinpirole injection; twice weekly for 8 pairs of injections) prevents Quinpirole-induced increases in dopamine D2-like receptor density in the nucleus accumbens and shifts quinpirole-induced behavioral sensitization from locomotion to 7-fold higher self-directed mouthing activity[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Long-Evans (male, 200-230 g at study start)[1]
Dosage: 1 mg/kg
Administration: s.c.; 90 minutes prior to each quinpirole injection; twice weekly for 8 pairs of injections
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.
Molecular Weight

265.31

Formula

C12H12FN3OS

CAS No.
SMILES

O=C(NCCN)C=1N=CSC1C=2C=CC=C(F)C2

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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Ro 41-1049
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HY-100027
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