Drug intelligence / Profile preview

[11C]-MDL100907

Development stage
Unknown
Lead developer
Lundbeck
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

**[11C]-MDL100907** is a radiolabeled form of MDL 100907 (volinanserin), a potent and highly selective competitive antagonist of the serotonin 2A (5-HT2A) receptor, used primarily as a positron emission tomography (PET) tracer for quantification and mapping of 5-HT2A receptors in the human and non-human primate brain in vivo. The compound demonstrates subnanomolar affinity for 5-HT2A (Ki ≈ 0.36 nM; KD ≈ 0.1 nM), over 80-fold selectivity for 5-HT2A relative to other serotonergic receptors, and negligible affinity for dopamine, adrenergic, muscarinic, or benzodiazepine receptors. [11C]-MDL100907 has been extensively characterized for its plasma kinetics, regional brain uptake, and ability to bind specifically to cortical 5-HT2A receptor sites, making it the most selective PET radiotracer for this molecular target currently available. Its application is research-based, enabling noninvasive in vivo studies of serotonergic function related to neuropsychiatric conditions[2][4][1].

Other names
volinanserin(R)-(+)-α-(2,3-Dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperinemethanol4-piperidinemethanol, alpha-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-, (alphaR)-CAS 139290-65-6CAS139290-65-6CAS-139290-65-6
02

Targets

HTR2A (Serotonin receptor 5-HT2A)

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