Delving into the Latest Updates on 18F-NS-14490 with Synapse

Overview

Basic Info

Drug Type

Diagnostic radiopharmaceuticals

Synonyms

Fluorine [18F ]-NS14490

+ [1]

Target

nAChRs

Mechanism

Nicotinic receptors modulators

Therapeutic Areas

Cardiovascular Diseases

Active Indication

AtherosclerosisMyocardial Infarction

Inactive Indication-

Originator Organization

DanPET AB

Active Organization

DanPET AB

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Structure

Molecular FormulaC19H22FN5O

InChIKeyZRTUGMRLPXGKGZ-LRFGSCOBSA-N

CAS Registry1236036-15-9

[(18)F]NS14490, a new potential radiotracer for neuroimaging of α7 nicotinic acetylcholine receptors (α7 nAChRs), was synthesized and evaluated in vitro and in vivo. Radioligand binding studies using [(3)H]methyllycaconitine and NS14490 as competitor showed a good target affinity (K(i,α7) = 2.5 nM) and a high selectivity towards other nAChRs. Radiosynthesis of [(18)F]NS14490 was performed by two different labelling procedures: a two-step synthesis using a prosthetic group, which led to 7% labelling yield, and the convenient direct nucleophilic substitution of the corresponding tosylate precursor, which resulted in 70% labelling yield. After optimisation of the isolation, purification and formulation process, biodistribution studies were performed in CD-1 mice. The brain uptake of [(18)F]NS14490 was comparably low (0.16% ID g(-1) wet weight at 5 min p.i.). The radiotracer showed a high metabolic stability in plasma and brain. Also, the target specificity was proven by pre-administration of a highly affine α7 ligand providing a rationale basis for further in vivo evaluation.

100 Deals associated with 18F-NS-14490

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