Target density (Bmax) of major CNS targets

To be completed......

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Target (abbreviated) Target (full name) Bmax references comments
β-Amyloid plaque 1000-2000 nM in human Alzheimer's disease J Neurosci., 2005, 16, 10598. PIB Kd = 2 nM
nAChR nicotinic cholinergic receptor

0.4-8 nM human brain (no details in subtypes)

similar to rodent brain

Nucl Med Biol 2006, 33, 449.

citing the following refs

human: Prog Neurobiol, 1997, 53, 199.

Behav Brain Res., 2000, 113, 143.

rodent: Neuropharm, 1993, 32, 847.

 

"This is a very-low-density site..." from Nucl Med Biol 2006, 33, 449.
AMPA α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid 148 fmol/mg (rat) BMC, 2006, 14, 4712. [3H]compound 1 in rat cortex
    200-1500 fmol/mg (rat) Brain Res, 1987, 402, 243 [3H]AMPA in rat brain; Best fit by two bind sites: (Bmax1 = 200 and Bmax2 = 1500); A single site fit gives Bmax = 1800
    1000 fmol/mg (rat) J Neurochem, 1998, 71, 418. [3H]Ro-48-8587 in rat whole brain;  high uptakes in cortical layers, hippocampus, striatum, dorsal septum, reticular thalamic nucleus. 
    7000 fmol/mg (rat) Mol. Pharmacol., 2000, 58, 1310. [3H]CP-526,427 in rat forebrain
CB1 cannabinoid receptor type 1 45 - 240 fmol/mg 

(adolescent rat brain)

Synapse, 2010, 64, 845. [3H]CP55,940; high regions: globus pallidus,lateral caudate putamen and substantia; low regions: retrosplenial cortex, olfactory tubercle and thalamus
D2 dopamine receptor D2

monkey

putamen 27 nM; caudate 23 nM; striatum 14 nM; thalamus 1.8 nM; amygdala 0.9 nM

Monkey:

J Cereb Blood Flow Metab., 2004, 24, 309.

fallypride Kd = 0.03nM in vitro
DAT dopamine transporter 2000 fmol/mg (rat striatum) Nucl Med Biol 2006, 33, 449.  
FAAH fatty acid amide hydrolase

43 nM (rat cortex); 21 nM (rehsus cortex); 15 nM (human cortex)

ACS Med Chem Lett, 2013, 4, 509. [3H]MK3168; reversible tracer
GABAA gamma-aminobutyric acid type A

rat whole brain determined by [35S]TBPS: 820-1610 fmol/mg

rat whole brain determined by [3H]Ro-15-1788: 1000-1190 fmol/mg

rat whole brain determined by [3H]muscimol: 1370-1500 fmol/mg

rat cortex and cerebellum by [35S]TBPS: 1560 and 1250 fmol/mg

human cortex and cerebellum by [35S]TBPS: 790 and 740 fmol/mg

Br J Pharmacol, 2007, 150, 1066. bmax range was profiled in 0, 5, 10 and 20 day post mortem delay.
         
mGluR1 metabotropic glutamate receptor 1

rat: cortex (47 nM); hippocampus (69 nM); striatum (74 nM); cerebellum (430 nM)

Rhesus monkey: cortex (10 nM); cerebellum (53 nM)

human: cortex (26 nM) and cerebellum (82 nM)

Curr Med Chem, 2014, 21, 113.

[3H]R214127 for rat brain

[18F]MK-1312 (allosteric antagonist) for monkey and human brain

mGluR5 metabotropic glutamate receptor 5 Rhesus monkey: caudate (63 nM) and cerebellum (24 nM) Synapse, 2005, 56, 205. [3H]1a (M-MTEB), mGluR5 antagonist, in the ref.
   

rat:

caudate/putamen: 83 fmol/mg

frontal cortex: 65 fmol/mg

hippocampus: 55 fmol/mg

thalamus: 40 fmol/mg

hypothalamus: 21 fmol/mg

Life Sci., 2003, 73, 371 [3H]MethoxyPyEP
H3R Histamine H3 receptor

Rhesus monkey striatum: 1.42 nM

human cortex/caudate/putamen

0.81 nM

Synapse, 2009, 63, 1122. [3H]1a, an inverse agonist, in the ref.

HDAC

histone deacetylase 12900 fmol/mg averaged over whole brain sections Epigentics, 2013, 8, 756. [3H]CI-994
NET norepinephrine transporter 55 fmol/mg (rat frontal cortex) Nucl Med Biol 2006, 33, 449.  
PDE4 phosphodiesterase 4

445 fmol/mg (mouse cortex)

107 fmol/mg (NHP cortex)

J Med Chem, 2017, 60, 8538. [3H]rolipram
   

488 fmol/mg (mouse cortex)

62 fmol/mg (NHP cortex)

J Med Chem, 2017, 60, 8538. [3H]PDE4B-preferring compound
         
PDE10A phosphodiesterase 10A

2200 fmol/mg (rat STR)

1000 fmol/mg (baboon R-STR)

1200 fmol/mg (human male putamen)

1400 fmol/mg (human female putamen)

 

JPET, 2015, 352, 327-337. [3H]AMG 580
    0.75 nM (rat striatum homogenate) J. Neurochemistry, 2016, 139, 897-906. [18F]JNJ42259152
    3990 fmol/mg (rat striatal membranes)

Pharmacological characterization of RO5461861, a potent and selective PDE10A inhibitor (poster)

  • November 2014
  • Conference: Society of Neuroscience Annual Meeting
  • At: Washington
[3H]RO5461861
    7200 fmol/mg (SD rat striatal homogenate) Pharma Res Per, 4(4), 2016, e00241,
doi: 10.1002/prp2.241
[3H]PDM-042
SERT serotonin transporter 194 fmol/mg (rat frontal cortex) Nucl Med Biol 2006, 33, 449.  
tau   3872-5823 fmol/mg (human AD brain) J Med Chem, 2017, in press. compounds [3H]7 and [3H]39 were used.
    Bmax1 = 250 fmol/mg; Bmax2 = 1416 fmol/mg from temporal lobe brain homogenates from AD patients Acta Neuropathol Commun 2015, 3, 40. [3H]THK5117
TRPV1

Transient Receptor Potential Vanilloid Subfamily Member 1

420-1050 fmol/mg (rat spinal cord); 16-42 fmol/mg (estimated brain level)

J. Mol. Neurosci, 2013, 50, 23 (spinal cord by ELISA method).

ACS Chem Neurosci, 2013, 4, 624 (brain estimation)

by ELISA method
         
TSPO translocator protein 18kDa 3930 fmol/ml (rat heart); 1410 fmol/ml (rat Lung); 1580 fmol/ml (rat kidney) NMB, 2010, 37, 853. [18F]FEDAC
    1038 fmol/mg (mouse cerebral cortex membranes) Brain, 2004, 127, 1379. [3H]PK11195
   

MS human brain

[3H]PK11195 (only single site binding)

HAB: 4325 fmol/mg; LAB 5063 fmol/mg.

[3H]PBR28 (single site model)

HAB: 1929 fmol/mg; LAB: 994 fmol/mg

[3H]PBR28 (two site model)

for both: 1861 fmol/mg

JCBFM, 2010, 30, 1608.

[3H]PK11195 and [3H]PBR28 on human brain tissues: Of the 22 donors, 20 had been diagnosed with MS, and 2 were control donors without MS.

MS = multiple sclerosis

HAB = high affinity binders

LAB = low affinity binders

   

Determined by [3H]PK11195

normal human brain:

gray matter 700 fmol/mg; white matter 400 fmol/mg

Glioblastroma:

proliferative zone 7600 fmol/mg; necrotic zone 1600 fmol/mg

Acta Neurochir (Wien), 1992, 119, 146. [3H]PK11195