Source 1primary paper2018Journal of Controlled Release
Toolkit/MRS7145
MRS7145
Taxonomy: Mechanism Branch / Architecture. Workflows sit above the mechanism and technique branches rather than replacing them.
Summary
The web research summary states that the anchor paper describes MRS7145 as the first light-dependent adenosine A2A receptor antagonist and identifies it as the photo-controlled/photocaged adenosine A2A receptor antagonist used for light-dependent blockade in cells and behaving animals.
Usefulness & Problems
Why this is useful
MRS7145 is described as a photoactive or photocaged adenosine A2A receptor antagonist that enables light-dependent receptor blockade. The anchor study uses it to remotely control movement-related phenotypes.; light-dependent antagonism of adenosine A2A receptor signaling; remote optical control of movement-related phenotypes in rodent models
Source:
MRS7145 is described as a photoactive or photocaged adenosine A2A receptor antagonist that enables light-dependent receptor blockade. The anchor study uses it to remotely control movement-related phenotypes.
Source:
light-dependent antagonism of adenosine A2A receptor signaling
Source:
remote optical control of movement-related phenotypes in rodent models
Problem solved
It addresses the need to restrict A2A receptor antagonism in space and time rather than applying conventional systemic antagonists without optical control.; enables spatially and temporally controlled A2A receptor antagonism
Source:
It addresses the need to restrict A2A receptor antagonism in space and time rather than applying conventional systemic antagonists without optical control.
Source:
enables spatially and temporally controlled A2A receptor antagonism
Problem links
enables spatially and temporally controlled A2A receptor antagonism
LiteratureIt addresses the need to restrict A2A receptor antagonism in space and time rather than applying conventional systemic antagonists without optical control.
Source:
It addresses the need to restrict A2A receptor antagonism in space and time rather than applying conventional systemic antagonists without optical control.
Published Workflows
Objective: Use a photoactive adenosine A2A receptor antagonist to achieve remote optical control of movement-related phenotypes in rodent models.
Why it works: The provided summary indicates that the compound is inactive or constrained until light exposure enables local receptor blockade, allowing optical control in rodent striatum and behavioral modulation.
adenosine A2A receptor antagonismphotouncagingin vitro receptor blockade assayin vivo optical pharmacology
Stages
- 1.In vitro receptor blockade(functional_characterization)
The summary indicates that receptor blockade was shown in vitro before in vivo photouncaging, supporting receptor-level function prior to behavioral application.
Selection: Demonstration of light-dependent adenosine A2A receptor blockade in vitro.
- 2.In vivo photouncaging in rodent striatum(in_vivo_validation)
This stage tests whether the photoactive antagonist can control movement-related phenotypes in a living animal after local light delivery.
Selection: Ability of local photouncaging in rodent striatum to modulate locomotion and parkinsonian-like behaviors.
Steps
- 1.Test MRS7145 for light-dependent A2A receptor blockade in vitrophotoactive antagonist being evaluated
Establish receptor-level light-dependent antagonism before animal testing.
The summary presents in vitro receptor blockade before in vivo photouncaging, implying an earlier lower-complexity validation step.
- 2.Apply in vivo photouncaging in rodent striatum and assess movement-related behaviorsphotoactive antagonist used for local optical activation
Determine whether local light-triggered A2A receptor antagonism can modulate locomotion and parkinsonian-like behaviors in vivo.
This follows receptor-level testing to evaluate behavioral efficacy in a higher-fidelity animal context.
Taxonomy & Function
Primary hierarchy
Mechanism Branch
Architecture: A reusable architecture pattern for arranging parts into an engineered system.
Techniques
No technique tags yet.
Target processes
No target processes tagged yet.
Input: Light
Implementation Constraints
cofactor dependency: cofactor requirement unknownencoding mode: genetically encodedimplementation constraint: context specific validationimplementation constraint: spectral hardware requirementoperating role: sensorswitch architecture: uncaging
Its use requires light delivery and an assay or animal preparation in which A2A receptor antagonism can be measured. The summary also indicates use in rodent striatum for in vivo photouncaging.; requires light delivery for activation or uncaging; requires an experimental system with adenosine A2A receptor readout
The provided evidence does not show that it solves broader delivery, tissue penetration, or clinical translation constraints. No direct comparison to standard antagonists is given in the supplied source text.; the provided evidence does not specify synthesis details, reversibility, or quantitative performance metrics
Validation
Cell-freeBacteriaMammalianMouseHumanTherapeuticIndep. Replication
Supporting Sources
Ranked Claims
MRS7145 is presented as a light-dependent adenosine A2A receptor antagonist used for in vitro receptor blockade and in vivo photouncaging.
The anchor paper is a 2018 primary study in Journal of Controlled Release describing MRS7145, presented as the first light-dependent adenosine A2A receptor (A2AR) antagonist, with in vitro receptor blockade and in vivo photouncaging in rodent striatum to modulate locomotion and parkinsonian-like behaviors.
The study reports remote control of movement disorders using a photoactive adenosine A2A receptor antagonist.
Remote control of movement disorders using a photoactive adenosine A2A receptor antagonist
Approval Evidence
1 source2 linked approval claimsfirst-pass slug mrs7145
The web research summary states that the anchor paper describes MRS7145 as the first light-dependent adenosine A2A receptor antagonist and identifies it as the photo-controlled/photocaged adenosine A2A receptor antagonist used for light-dependent blockade in cells and behaving animals.
Source:
mechanism or modalitysupports
MRS7145 is presented as a light-dependent adenosine A2A receptor antagonist used for in vitro receptor blockade and in vivo photouncaging.
The anchor paper is a 2018 primary study in Journal of Controlled Release describing MRS7145, presented as the first light-dependent adenosine A2A receptor (A2AR) antagonist, with in vitro receptor blockade and in vivo photouncaging in rodent striatum to modulate locomotion and parkinsonian-like behaviors.
Source:
tool capabilitysupports
The study reports remote control of movement disorders using a photoactive adenosine A2A receptor antagonist.
Remote control of movement disorders using a photoactive adenosine A2A receptor antagonist
Source:
Comparisons
Source-stated alternatives
The surrounding literature mentions comparator A2A antagonists including MSX-3, SCH58261, KW-6002, and istradefylline, and a related photopharmacology tool JF-NP-26 for mGlu5.
Source:
The surrounding literature mentions comparator A2A antagonists including MSX-3, SCH58261, KW-6002, and istradefylline, and a related photopharmacology tool JF-NP-26 for mGlu5.
Source-backed strengths
presented as the first light-dependent A2A receptor antagonist; reported to support both in vitro receptor blockade and in vivo photouncaging
Source:
presented as the first light-dependent A2A receptor antagonist
Source:
reported to support both in vitro receptor blockade and in vivo photouncaging
Compared with KnChR
MRS7145 and KnChR address a similar problem space.
Shared frame: same top-level item type; shared mechanisms: conformational_uncaging; same primary input modality: light
Strengths here: looks easier to implement in practice; may avoid an exogenous cofactor requirement.
Compared with light-regulated protein-protein interaction
MRS7145 and light-regulated protein-protein interaction address a similar problem space.
Shared frame: same top-level item type; shared mechanisms: conformational_uncaging; same primary input modality: light
Compared with o-nitrobenzyl-caged fluorescein conjugate
MRS7145 and o-nitrobenzyl-caged fluorescein conjugate address a similar problem space.
Shared frame: same top-level item type; shared mechanisms: conformational_uncaging; same primary input modality: light
Ranked Citations
- 1.