DAA-1106 is a drug which acts as a potent and selective
agonist at the
peripheral benzodiazepine receptor, also known as the mitochondrial 18 kDa translocator protein or TSPO, but with no affinity at the
GABAA receptor. It has
anxiolytic effects in animal studies.[1][2][3] DAA-1106 has a sub-nanomolar
binding affinity (Ki) of 0.28 nM, and has been used extensively in its 3H or 11C
radiolabelled form to map TSPO in the body and brain, which has proved especially helpful in monitoring the progress of neurodegenerative diseases such as
Alzheimer's disease.[4][5][6][7][8][9]
^Venneti S, Lopresti BJ, Wang G, Slagel SL, Mason NS, Mathis CA, Fischer ML, Larsen NJ, Mortimer AD, Hastings TG, Smith AD,
Zigmond MJ, Suhara T, Higuchi M, Wiley CA (September 2007). "A comparison of the high-affinity peripheral benzodiazepine receptor ligands DAA1106 and (R)-PK11195 in rat models of neuroinflammation: implications for PET imaging of microglial activation". Journal of Neurochemistry. 102 (6): 2118–31.
doi:
10.1111/j.1471-4159.2007.04690.x.
PMID17555551.
S2CID3788208.
^Doorduin J, de Vries EF, Dierckx RA, Klein HC (2008). "PET imaging of the peripheral benzodiazepine receptor: monitoring disease progression and therapy response in neurodegenerative disorders". Current Pharmaceutical Design. 14 (31): 3297–315.
doi:
10.2174/138161208786549443.
PMID19075709.
^Gulyás B, Makkai B, Kása P, Gulya K, Bakota L, Várszegi S, Beliczai Z, Andersson J, Csiba L, Thiele A, Dyrks T, Suhara T, Suzuki K, Higuchi M, Halldin C (January 2009). "A comparative autoradiography study in post mortem whole hemisphere human brain slices taken from Alzheimer patients and age-matched controls using two radiolabelled DAA1106 analogues with high affinity to the peripheral benzodiazepine receptor (PBR) system". Neurochemistry International. 54 (1): 28–36.
doi:
10.1016/j.neuint.2008.10.001.
PMID18984021.
S2CID21033494.
^Wang M, Gao M, Hutchins GD, Zheng QH (June 2009). "Synthesis of [11C]FEDAA1106 as a new PET imaging probe of peripheral benzodiazepine receptor expression". European Journal of Medicinal Chemistry. 44 (6): 2748–53.
doi:
10.1016/j.ejmech.2008.08.001.
PMID18790550.