(N-stearyl, Norleucine17)VIPhybrid is a broad spectrum vasoactive intestinal peptide receptor antagonist

Terry W. Moody; Robert T. Jensen; Mati Fridkin; Illana Gozes

doi:10.1385/JMN:18:1-2:29

(N-stearyl, Norleucine¹⁷)VIPhybrid is a broad spectrum vasoactive intestinal peptide receptor antagonist

Terry W. Moody^*, Robert T. Jensen, Mati Fridkin, Illana Gozes

^*Corresponding author for this work

Human Molecular Genetics Biochemistry

Research output: Contribution to journal › Article › peer-review

24 Scopus citations

Abstract

The effects of a (N-stearyl, Norleucine¹⁷) vasoactive intestinal peptide hybrid ((SN)VIPhybrid) on cells stably transfected with VPAC₁, VPAC₂, or PAC₁ receptors were investigated. (SN)VIPhybrid inhibited specific ¹²⁵I-VIP binding to membranes derived from CHO cells transfected with VPAC₁ or VPAC₂ receptors with high affinity (IC₅₀ = 30 and 50 nM). (SN)VIPhyb inhibited specific ¹²⁵I-PACAP-27 binding to membranes derived from NIH/3T3 cells transfected with PAC₁ receptors with high affinity (IC₅₀ = 65 nM). PACAP-27 caused cAMP elevation in NIH/3T3 cells transfected with PAC₁ receptors and the increase cAMP caused by pituitary adenylated cyclase (PACAP) was inhibited by (SN)VIPhyb. Also, the increase in cAMP caused by VIP using CHO cells transfected with VPAC₁ or VPAC₂ receptors was antagonized by (SN)VIPhyb. These results indicate that (SN)VIPhyb is an antagonist for VPAC₁, VPAC₂, and PAC₁ receptors.

Original language	English
Pages (from-to)	29-35
Number of pages	7
Journal	Journal of Molecular Neuroscience
Volume	18
Issue number	1-2
DOIs	https://doi.org/10.1385/JMN:18:1-2:29
State	Published - 2002

Keywords

Antagonist
Binding
Cyclic AMP (cAMP)
PACAP receptors
VIP receptors

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title = "(N-stearyl, Norleucine17)VIPhybrid is a broad spectrum vasoactive intestinal peptide receptor antagonist",

abstract = "The effects of a (N-stearyl, Norleucine17) vasoactive intestinal peptide hybrid ((SN)VIPhybrid) on cells stably transfected with VPAC1, VPAC2, or PAC1 receptors were investigated. (SN)VIPhybrid inhibited specific 125I-VIP binding to membranes derived from CHO cells transfected with VPAC1 or VPAC2 receptors with high affinity (IC50 = 30 and 50 nM). (SN)VIPhyb inhibited specific 125I-PACAP-27 binding to membranes derived from NIH/3T3 cells transfected with PAC1 receptors with high affinity (IC50 = 65 nM). PACAP-27 caused cAMP elevation in NIH/3T3 cells transfected with PAC1 receptors and the increase cAMP caused by pituitary adenylated cyclase (PACAP) was inhibited by (SN)VIPhyb. Also, the increase in cAMP caused by VIP using CHO cells transfected with VPAC1 or VPAC2 receptors was antagonized by (SN)VIPhyb. These results indicate that (SN)VIPhyb is an antagonist for VPAC1, VPAC2, and PAC1 receptors.",

keywords = "Antagonist, Binding, Cyclic AMP (cAMP), PACAP receptors, VIP receptors",

author = "Moody, {Terry W.} and Jensen, {Robert T.} and Mati Fridkin and Illana Gozes",

year = "2002",

doi = "10.1385/JMN:18:1-2:29",

language = "אנגלית",

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AU - Moody, Terry W.

AU - Jensen, Robert T.

AU - Fridkin, Mati

AU - Gozes, Illana

PY - 2002

Y1 - 2002

N2 - The effects of a (N-stearyl, Norleucine17) vasoactive intestinal peptide hybrid ((SN)VIPhybrid) on cells stably transfected with VPAC1, VPAC2, or PAC1 receptors were investigated. (SN)VIPhybrid inhibited specific 125I-VIP binding to membranes derived from CHO cells transfected with VPAC1 or VPAC2 receptors with high affinity (IC50 = 30 and 50 nM). (SN)VIPhyb inhibited specific 125I-PACAP-27 binding to membranes derived from NIH/3T3 cells transfected with PAC1 receptors with high affinity (IC50 = 65 nM). PACAP-27 caused cAMP elevation in NIH/3T3 cells transfected with PAC1 receptors and the increase cAMP caused by pituitary adenylated cyclase (PACAP) was inhibited by (SN)VIPhyb. Also, the increase in cAMP caused by VIP using CHO cells transfected with VPAC1 or VPAC2 receptors was antagonized by (SN)VIPhyb. These results indicate that (SN)VIPhyb is an antagonist for VPAC1, VPAC2, and PAC1 receptors.

AB - The effects of a (N-stearyl, Norleucine17) vasoactive intestinal peptide hybrid ((SN)VIPhybrid) on cells stably transfected with VPAC1, VPAC2, or PAC1 receptors were investigated. (SN)VIPhybrid inhibited specific 125I-VIP binding to membranes derived from CHO cells transfected with VPAC1 or VPAC2 receptors with high affinity (IC50 = 30 and 50 nM). (SN)VIPhyb inhibited specific 125I-PACAP-27 binding to membranes derived from NIH/3T3 cells transfected with PAC1 receptors with high affinity (IC50 = 65 nM). PACAP-27 caused cAMP elevation in NIH/3T3 cells transfected with PAC1 receptors and the increase cAMP caused by pituitary adenylated cyclase (PACAP) was inhibited by (SN)VIPhyb. Also, the increase in cAMP caused by VIP using CHO cells transfected with VPAC1 or VPAC2 receptors was antagonized by (SN)VIPhyb. These results indicate that (SN)VIPhyb is an antagonist for VPAC1, VPAC2, and PAC1 receptors.

KW - Antagonist

KW - Binding

KW - Cyclic AMP (cAMP)

KW - PACAP receptors

KW - VIP receptors

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JF - Journal of Molecular Neuroscience

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ER -

(N-stearyl, Norleucine¹⁷)VIPhybrid is a broad spectrum vasoactive intestinal peptide receptor antagonist

Abstract

Keywords

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