McN5652 explained

McN5652[1] is a molecule that can be radiolabeled and then used as a radioligand in positron emission tomography (PET) studies. The [11C]-(+)-McN5652 enantiomer binds to the serotonin transporter.[2] The radioligand is used for molecular neuroimaging and for imaging of the lungs.[3]

It was developed by Johnson & Johnson's McNeil Laboratories. According to McNeil, McN5652 was among the strongest SRI ever reported at the time of its discovery (sub nM Ki). However, it is not completely 5-HT selective: the racemate has 5-HT=0.68, NA=2.9, and D=36.8nM, whereas (+)-enantiomer has 5-HT=0.39, NA=1.8, and D=23.5 nM. Paroxetine was listed as 5-HT=0.44 nM, NA=20, and DA=460nM in the same paper by the same authors.

Derivatives

McN5652 and related structures have been analyzed for QSAR in terms of binding to the MAT receptor binding site.[4]

See also

Notes and References

  1. US 4595688 Certain Hexahydro-6-Arylprylpyrrolo [2,1-A]Isoquinoline
  2. M. Suehiro . U. Scheffel . H. T. Ravert . R. F. Dannals . H. N. Jr Wagner . [11C](+)McN5652 as a radiotracer for imaging serotonin uptake sites with PET . Life Sciences . 53 . 11 . 883–92 . 1993 . 8366755 . 10.1016/0024-3205(93)90440-E. free .
  3. Akihiro Takano . Hiroshi Ito . Yasuhiko Sudo . Makoto Inoue . Tetsuya Ichimiya . Fumihiko Yasuno . Kazutoshi Suzuki . Tetsuya Suhara . Effects of smoking on the lung accumulation of [11C]McN5652 . Annals of Nuclear Medicine . 21 . 6 . 349–54 . August 2007 . 10.1007/s12149-007-0031-1 . 17705015. 43751275 .
  4. Liu. Shuang. Zha. Congxiang. Nacro. Kassoum. Hu. Min. Cui. Wenge. Yang. Yuh-Lin. Bhatt. Ulhas. Sambandam. Aruna. Isherwood. Matthew. Yet. Larry. Herr. Michael T.. Ebeltoft. Sarah. Hassler. Carla. Fleming. Linda. Pechulis. Anthony D.. Payen-Fornicola. Anne. Holman. Nicholas. Milanowski. Dennis. Cotterill. Ian. Mozhaev. Vadim. Khmelnitsky. Yuri. Guzzo. Peter R.. Sargent. Bruce J.. Molino. Bruce F.. Olson. Richard. King. Dalton. Lelas. Snjezana. Li. Yu-Wen. Johnson. Kim. Molski. Thaddeus. Orie. Anitra. Ng. Alicia. Haskell. Roy. Clarke. Wendy. Bertekap. Robert. O’Connell. Jonathan. Lodge. Nicholas. Sinz. Michael. Adams. Stephen. Zaczek. Robert. Macor. John E.. Design and Synthesis of 4-Heteroaryl 1,2,3,4-Tetrahydroisoquinolines as Triple Reuptake Inhibitors. ACS Medicinal Chemistry Letters. 5. 7. 2014. 760–765. 1948-5875. 10.1021/ml500053b. 25050161. 4094255.

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