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Cat. No.: HY-100027

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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.

For research use only. We do not sell to patients.

CAS No.: 127500-84-9
Formula: C₁₂H₁₂FN₃OS
Molecular Weight:265.31

Storage:

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

Ro 41-1049 Chemical Structure

CAS No.: 127500-84-9

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
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Biological Activity

Description

IC₅₀ & Target

^[1]

D₂ Receptor

MAO-A

All Monoamine Oxidase Isoforms :

MAO-A
MAO-B

All Dopamine Receptor Isoforms :

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 (K_d = 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.

Chemical Information

CAS No. 127500-84-9
Molecular Weight 265.31
Formula C₁₂H₁₂FN₃OS
SMILES

O=C(NCCN)C=1N=CSC1C=2C=CC=C(F)C2
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Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Culver KE, et al.. Altered dopamine D2-like receptor binding in rats with behavioral sensitization to quinpirole: effects of pre-treatment with Ro 41-1049. European journal of pharmacology. 2008 Sep 11;592(1-3):67-72. [Content Brief]

[2]. Saura J, et al. Quantitative enzyme radioautography with 3H-Ro 41-1049 and 3H-Ro 19-6327 in vitro: localization and abundance of MAO-A and MAO-B in rat CNS, peripheral organs, and human brain[J]. Journal of Neuroscience, 1992, 12(5): 1977-1999.

[3]. Da Prada M, et al. From moclobemide to Ro 19-6327 and Ro 41-1049: the development of a new class of reversible, selective MAO-A and MAO-B inhibitors[C]//Neurotransmitter Actions and Interactions: Proceedings of a Satellite Symposium of the 12th International Society for Neurochemistry Meeting, Algarve, Portugal, April 29–30, 1989. Vienna: Springer Vienna, 1990: 279-292.

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How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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Ro 41-1049

All Monoamine Oxidase Isoforms

All Dopamine Receptor Isoforms