The role of hydrophobic interactions in binding of polyamines to non NMDA receptor ion channels.

C Cu; Robert Bähring; M L Mayer; C Cui

The role of hydrophobic interactions in binding of polyamines to non NMDA receptor ion channels.

Standard

The role of hydrophobic interactions in binding of polyamines to non NMDA receptor ion channels. / Cu, C; Bähring, Robert; Mayer, M L; Cui, C.

In: NEUROPHARMACOLOGY, Vol. 37, No. 10-11, 10-11, 1998, p. 1381-1391.

Research output: SCORING: Contribution to journal › SCORING: Journal article › Research › peer-review

Harvard

Cu, C, Bähring, R, Mayer, ML & Cui, C 1998, 'The role of hydrophobic interactions in binding of polyamines to non NMDA receptor ion channels.', NEUROPHARMACOLOGY, vol. 37, no. 10-11, 10-11, pp. 1381-1391. <http://www.ncbi.nlm.nih.gov/pubmed/9849673?dopt=Citation>

APA

Cu, C., Bähring, R., Mayer, M. L., & Cui, C. (1998). The role of hydrophobic interactions in binding of polyamines to non NMDA receptor ion channels. NEUROPHARMACOLOGY, 37(10-11), 1381-1391. [10-11]. http://www.ncbi.nlm.nih.gov/pubmed/9849673?dopt=Citation

Vancouver

Cu C, Bähring R, Mayer ML, Cui C. The role of hydrophobic interactions in binding of polyamines to non NMDA receptor ion channels. NEUROPHARMACOLOGY. 1998;37(10-11):1381-1391. 10-11.

Bibtex

@article{62ec36b8a3cf4300923909a286001446,

title = "The role of hydrophobic interactions in binding of polyamines to non NMDA receptor ion channels.",

abstract = "Block of kainate subtype glutamate receptor channels by internal polyamines was analysed using outside out patches from HEK 293 cells transiently transfected with GluR6(Q). Tetramines with different numbers and spacing of methylene groups between NH2 groups produced biphasic rectification well fit by the Woodhull model for a weakly permeable ion channel blocker. Such analysis revealed an increase in binding energy of 611 cal M(-1) for each methylene group added over the range 6-12 (CH2), suggesting that a major component of block by polyamines involves hydrophobic binding. Isomers with the same number of CH2 groups but different spacing between NH2 groups showed similar affinity. Due to differences in pKa values for protonation of NH2 groups, the average charge on the tetramines studied would be expected to vary from 3.98 to 2.22 at physiological pH; despite this, the voltage dependence of block was similar for all tetramines tested, with a mean value for ztheta of 1.82, similar to values for polyamines with five or six NH2 groups. In contrast, for 1,3-propane diamine (DA3 ztheta 0.83), and the N-propyl- (ztheta 1.42) and N,N'-diethyl- (ztheta 1.37) analogues of DA3, there was an increase in the voltage dependence of block on addition of hydrophobic groups.",

author = "C Cu and Robert B{\"a}hring and Mayer, {M L} and C Cui",

year = "1998",

language = "Deutsch",

volume = "37",

pages = "1381--1391",

journal = "NEUROPHARMACOLOGY",

issn = "0028-3908",

publisher = "Elsevier Limited",

number = "10-11",

}

RIS

TY - JOUR

T1 - The role of hydrophobic interactions in binding of polyamines to non NMDA receptor ion channels.

AU - Cu, C

AU - Bähring, Robert

AU - Mayer, M L

AU - Cui, C

PY - 1998

Y1 - 1998

N2 - Block of kainate subtype glutamate receptor channels by internal polyamines was analysed using outside out patches from HEK 293 cells transiently transfected with GluR6(Q). Tetramines with different numbers and spacing of methylene groups between NH2 groups produced biphasic rectification well fit by the Woodhull model for a weakly permeable ion channel blocker. Such analysis revealed an increase in binding energy of 611 cal M(-1) for each methylene group added over the range 6-12 (CH2), suggesting that a major component of block by polyamines involves hydrophobic binding. Isomers with the same number of CH2 groups but different spacing between NH2 groups showed similar affinity. Due to differences in pKa values for protonation of NH2 groups, the average charge on the tetramines studied would be expected to vary from 3.98 to 2.22 at physiological pH; despite this, the voltage dependence of block was similar for all tetramines tested, with a mean value for ztheta of 1.82, similar to values for polyamines with five or six NH2 groups. In contrast, for 1,3-propane diamine (DA3 ztheta 0.83), and the N-propyl- (ztheta 1.42) and N,N'-diethyl- (ztheta 1.37) analogues of DA3, there was an increase in the voltage dependence of block on addition of hydrophobic groups.

AB - Block of kainate subtype glutamate receptor channels by internal polyamines was analysed using outside out patches from HEK 293 cells transiently transfected with GluR6(Q). Tetramines with different numbers and spacing of methylene groups between NH2 groups produced biphasic rectification well fit by the Woodhull model for a weakly permeable ion channel blocker. Such analysis revealed an increase in binding energy of 611 cal M(-1) for each methylene group added over the range 6-12 (CH2), suggesting that a major component of block by polyamines involves hydrophobic binding. Isomers with the same number of CH2 groups but different spacing between NH2 groups showed similar affinity. Due to differences in pKa values for protonation of NH2 groups, the average charge on the tetramines studied would be expected to vary from 3.98 to 2.22 at physiological pH; despite this, the voltage dependence of block was similar for all tetramines tested, with a mean value for ztheta of 1.82, similar to values for polyamines with five or six NH2 groups. In contrast, for 1,3-propane diamine (DA3 ztheta 0.83), and the N-propyl- (ztheta 1.42) and N,N'-diethyl- (ztheta 1.37) analogues of DA3, there was an increase in the voltage dependence of block on addition of hydrophobic groups.

M3 - SCORING: Zeitschriftenaufsatz

VL - 37

SP - 1381

EP - 1391

JO - NEUROPHARMACOLOGY

JF - NEUROPHARMACOLOGY

SN - 0028-3908

IS - 10-11

M1 - 10-11

ER -