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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