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Table 1 The transportability of peptidic compounds across the blood-brain barrier

From: A trip of peptides to the brain

Penetrant Cell or animal Influx or efflux Time Data Doi
cyclo(Phe-Phe) cell influx 20, 40, 60 min Papp = ~25 ×10-6 cm/s doi:10.1371/journal.pone.0050824
Pro-HyPa rat influx 30 min ~0.5 nmol/mL-cerebrospinal fluid (ginger-degraded collagen hydrolysate 600 mg/kg p.o.) doi:10.1096/fj.201902871R
Trp-Tyr rat influx 2 h tissue/plasma ratio : 0.23 (hippocampus) doi:10.18632/aging.101909
Leu-His rat influx 2 h tissue/plasma ratio : 0.19 (hippocampus) doi:10.3390/nu11092161
Met-Lys-Pro rat influx 15 min autoradiographic image doi:10.1371/journal.pone.0171515
Gly-Sar mouse brain slice influx 10 min Uptake = ~110 μL/g (hippocampus) doi:10.1111/jnc.12687
cyclo(His-Pro) mousse (i.v) influx 120 min Ki = 0.179 μL/g-min doi:10.1152/ajpendo.1993.264.5.E723
kyotorphin ( Tyr-Arg ) mouse (i.c.v.) efflux 2-15 min t1/2 = 4.9 min doi:10.1111/j.1471-4159.2009.06090.x
histidine mouse brain slice influx 3 min Uptake = ~0.09 μL/g (hippocampus) doi:10.1016/j.bcp.2016.11.012
mouse(1 nmol/g : i.v) influx 0~30 min concentration = ~0.5 nmol/g(hippocampus) doi:10.1016/j.bcp.2016.11.012
oxytocin [ CYINQCPLG ( Disulfide bridge: 1-6 ) ] cell influx 3 h Papp = 3.03 ×10-6 cm/s doi:10.1038/s42003-019-0325-6
neuropeptide Y mouse influx 2-30 min Ki = 0.194 μL/g-min doi:10.1152/ajpendo.1999.276.3.E479
endomorphin rat influx 15-60 min HPLC Chromatogram doi:10.1016/j.regpep.2005.12.004
alanine mouse influx 5 min Papp = 9.6± 0.8 ×10-6 cm/s doi:10.1016/j.tiv.2004.06.011
L-dopa mouse influx 5 min Papp = 3.9± 0.79 ×10-6 cm/s doi:10.1016/j.tiv.2004.06.011
leucine mouse influx 5 min Papp = 14.6± 1.9 ×10-6 cm/s doi:10.1016/j.tiv.2004.06.011
apolipoprotein J mouse influx 1.0 - 10 min Ki = 3.75 μL/g-min doi:10.1016/s0024-3205(96)00685-6
SAM 995 ( Tyr-D-Thr-Gly-Phe-Leu-Ser ) rat influx 5.0 - 20 min Ki = 1.0 ± 0.2 μL/g-min http://jpet.aspetjournals.org/content/299/3/967
SAM 1095 ( O-linked Ser6-β-D-glucose analog of SAM995 ) rat influx 5.0 - 20 min Ki = 2.2 ± 0.3 μL/g-min http://jpet.aspetjournals.org/content/299/3/967
DPDPE ( Tyr-D-penicillamine-Gly-Phe-D-penicillamine ) rat influx 30 min Ki = 1.46 ± 0.31 μL/g-min doi:10.1046/j.1471-4159.1996.66031289.x
valproic acid rat influx 0.25 - 0.5 min Ki = ~ 480 μL/g-min http://jpet.aspetjournals.org/content/276/3/1189
amantadin mouse influx 10 - 20 sec Ki = 102 μL/g-min doi:10.1002/bdd.2014
clonidine mouse influx 0.5 - 3.0 min Ki = 366 μL/g-min doi:10.1038/jcbfm.2009.54
  1. aHyP hydroxyl Pro