458567-42-5

Upstream product

• 506-68-3 bromocyane 
• 1783-81-9 3-methylmercaptoaniline 
• 71205-41-9 1-(3-(methylthio)phenyl)thiourea 

Downstream Products

• 222734-73-8 N-methyl-N-(3-(methylthio)phenyl)cyanamide 
• 160754-78-9 N-(2-chloro-5-(methylthio)phenyl)-N'-(3-(methylthio)phenyl)guanidine 
• 917894-23-6 N-(2-chloro-5-mercaptophenyl)-N'-methyl-N'-(3-thiomethylphenyl)guanidine 
• 917894-05-4 N-(2-chloro-5-fluoromethylthiophenyl)-N'-(3-methylthiophenyl)-N'-methyl-guanidine 
• 917894-11-2 N-(2-chloro-5-(S-2-fluoroethyl)thiophenyl)-N'-(3-methylthiophenyl)-N'-methyl guanidine 
• 917894-09-8 N-(2-chloro-5-mercaptophenyl)-N'-(3-methylthiophenyl)-N'-methyl-guanidine hydrochloride 
• 1349064-27-2 1,1’-(disulfanediylbis(6-chloro-1,3-phenylene))bis(3-methyl-3-(3-(methylthio)phenyl)guanidine) 

Relevant academic research and scientific papers

Synthesis and in vitro evaluation of N,N'-diphenyl and N-naphthyl-N'-phenylguanidines as N-methyl-D-aspartate receptor ion-channel ligands.

A series of N,N'-diphenyl and N-naphthyl-N'-phenyl guanidine derivatives was synthesized as potential N-methyl-D-aspartate (NMDA) receptor positron emission tomography (PET) ligands. The affinity of the different compounds was determined using in vitro receptor binding assays, and their log P values were estimated using HPLC analysis. The effect of N'-3 and N'-3,5 substitution on affinity and lipophilicity was examined. The K(i) values ranged from 1.87 to 839nM, while log P values between 1.22 and 2.88 were observed.

Development of an automated, GMP compliant FASTlab radiosynthesis of [18F]GE-179 for the clinical study of activated NMDA receptors

N-(2-chloro-5-(S-2-[18F]fluoroethyl)thiophenyl)-N'-(3-thiomethylphenyl)-N'-methylguanidine, ([18F]GE-179), has been identified as a promising positron emission tomography (PET) ligand for the intra-channel phencyclidine (PCP) binding

Synthetic method of [18F]-GE-179

The invention discloses a [18F]-GE-179 synthesis method, which comprises: step 1, generating H protons by a cyclotron to bombard 18O heavy oxygen water, generating 18F ions by using a nuclearreaction 18O(p, n)18F; enriching the 18F ions throug

New N-aryl-N′-(3-(substituted)phenyl)-N′-methylguanidines as leads to potential PET radioligands for imaging the open NMDA receptor

An expansive set of N-aryl-N′-(3-(substituted)phenyl)-N′-methylguanidines was prepared in a search for new leads to prospective PET ligands for imaging of the open channel of the N-methyl-d-aspartate (NMDA) receptor in vivo. The N-aryl rings and their substituents were varied, whereas the N-methyl group was maintained as a site for potential labeling with the positron-emitter, carbon-11 (t1/2 = 20.4 min). At micromolar concentration, over half of the prepared compounds strongly inhibited the binding of [3H]TCP to its binding site in the open NMDA receptor in vitro. Four ligands displayed affinities that are similar or superior to those of the promising SPECT radioligand ([123I]CNS1261). The 3′-dimethylamino (19; Ki 36.7 nM), 3′-trifluoromethyl (20; Ki 18.3 nM) and 3′-methylthio (2; Ki 39.8 nM) derivatives of N-1-naphthyl-N′-(phenyl)-N′-methylguanidine were identified as especially attractive leads for PET radioligand development.

IMAGING 18F OR 11C-LABELLED ALKYLTHIOPHENYL GUANIDINES

The invention provides a compound of formula (I); or a salt or solvate thereof, wherein: R1 is hydrogen or C1-4alkyl; R2 and R4 are each independently selected from C1-4 alkyl, [11C] C1 4alkyl, and [18F]-C1-4 fluoroalkyl provided that at least one of R2 and R4 is [11C] C1 4alkyl or [18F]-C1-4 fluoroalkyl; and R3 is halo. Such compounds having use for imaging central nervous system receptors.

Synthesis and characterization of N-(2-chloro-5-methylthiophenyl)-N′- (3-methylthiophenyl)-N′-[11C]methylguanidine [ 11C]CNS 5161, a candidate PET tracer for functional imaging of NMDA receptors

N-methyl-D-aspartate (NMDA) receptors play a key role in excitatory neurotransmission and are linked to a variety of acute and chronic neurodegenerative diseases including epilepsy, schizophrenia, Parkinson's disease and drug abuse. N-(2-chloro-5-methylth

IMAGING COMPOUNDS

The invention relates to compounds of formula: (I) or a salt or solvate thereof, wherein: R1 is -11CH2R5 or [18F]-C1-4 fluoroalkyl wherein R5 is hydrogen or C1-4 alkyl