Chemistry:MADAM

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MADAM, also known as N,N-dimethyl-2-(2-amino-4-methylphenylthio)benzylamine, is a highly potent and selective serotonin reuptake inhibitor (SRI) which is used in scientific research.[1] Its affinity (Kd) for the serotonin transporter (SERT) is 60 pM (0.06 nM).[1] Radiolabeled isotopologues of MADAM have been developed and used as radiotracers in positron emission tomography (PET) imaging.[2][3][4][5] The drug was first described in the scientific literature by 2001.[6][7]

References

  1. ↑ 1.0 1.1 "Pharmacological characterization of N,N-dimethyl-2-(2-amino-4-methylphenyl thio)benzylamine as a ligand of the serotonin transporter with high affinity and selectivity". The Journal of Pharmacology and Experimental Therapeutics 304 (1): 81–87. January 2003. doi:10.1124/jpet.102.042226. PMID 12490578. 
  2. ↑ "Carbon-11 labelling of MADAM in two different positions: a highly selective PET radioligand for the serotonin transporter". Journal of Labelled Compounds and Radiopharmaceuticals 44 (14): 1013–1023. 2001. doi:10.1002/jlcr.523. ISSN 0362-4803. 
  3. ↑ "Selectivity of (3)H-MADAM binding to 5-hydroxytryptamine transporters in vitro and in vivo in mice; correlation with behavioural effects". British Journal of Pharmacology 141 (6): 1015–1023. March 2004. doi:10.1038/sj.bjp.0705693. PMID 14993096. 
  4. ↑ "[(11)C]MADAM, a new serotonin transporter radioligand characterized in the monkey brain by PET". Synapse (New York, N.Y.) 58 (3): 173–183. December 2005. doi:10.1002/syn.20189. PMID 16138320. 
  5. ↑ "Quantification of 11C-MADAM binding to the serotonin transporter in the human brain". Journal of Nuclear Medicine 46 (9): 1505–1515. September 2005. PMID 16157534. 
  6. ↑ "Pharmacological characterization of N, N-dimethyl-2 (2-amino-4-methylphenylthio) benzylamine or MADAM as a radioligand of the serotonin transporter with high affinity and selectivity". European Journal of Nuclear Medicine 28 (8): 997. August 2001. 
  7. ↑ "N,N-dimethyl-2-(2-amino-4-methylphenylthio) benzylamine or MADAM is a serotonin transporter ligand with high affinity and specificity: in vitro characterization". NeuroImage 16 (3): S18. July 2002.