A novel, selective radioligand, [125I]-[Lys5, Tyr(I2)7, Meleu9, Nle10]-NKA(4-10), for the tachykinin NK-2 receptor

Tim Badgery-Parker; Xiang-Ping Zeng; Solange Lavielle; Elizabeth Burcher

doi:10.1016/0167-0115(93)90118-R

A novel, selective radioligand, [¹²⁵I]-[Lys⁵, Tyr(I₂)⁷, Meleu⁹, Nle¹⁰]-NKA(4-10), for the tachykinin NK-2 receptor

Tim Badgery-Parker, Xiang-Ping Zeng, Solange Lavielle, Elizabeth Burcher^*

^*Corresponding author for this work

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

5 Citations (Scopus)

Abstract

A new radioligand, [¹²⁵I]-[Lys⁵Tyr(I₂)⁷,MeLeu⁹,Nle¹⁰]-NKA(4-10), based on the selective agonist [Lys⁵,MeLeu⁹,Nle¹⁰]-NKA(4-10) has been developed. Binding in rat fundus membranes was displaced by NP_γ>NKA≥[Lys⁵,MeLeu⁹,Nle¹⁰]-NKA(4-10)>neuropeptide K> Lys⁵,Tyr I₂MeLeu⁹,Nle¹⁰]-NKA(4-10)>SP> [Sar⁹,Met(O₂¹¹]-SP≫ senktide, indicating binding to NK-2 receptors. Preliminary studies demostrated high specific binding in membranes from rat urinary bladder, duodenum and colon. Specific binding in rat brain and lung was negligible, and binding in a range of guinea-pig tissues was no more than 35% specific. These data may indicate species differences in NK-2 receptors.

Original language	English
Pages (from-to)	455-457
Number of pages	3
Journal	Regulatory Peptides
Volume	46
Issue number	1-2
DOIs	https://doi.org/10.1016/0167-0115(93)90118-R
Publication status	Published - 2 Jul 1993
Externally published	Yes

Keywords

Neuropeptide γ
NK-2 receptor
Rat gastric fundus
Selective radioligand
Tachykinin

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10.1016/0167-0115(93)90118-R

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title = "A novel, selective radioligand, [125I]-[Lys5, Tyr(I2)7, Meleu9, Nle10]-NKA(4-10), for the tachykinin NK-2 receptor",

abstract = "A new radioligand, [125I]-[Lys5Tyr(I2)7,MeLeu9,Nle10]-NKA(4-10), based on the selective agonist [Lys5,MeLeu9,Nle10]-NKA(4-10) has been developed. Binding in rat fundus membranes was displaced by NPγ>NKA≥[Lys5,MeLeu9,Nle10]-NKA(4-10)>neuropeptide K> Lys5,Tyr I2MeLeu9,Nle10]-NKA(4-10)>SP> [Sar9,Met(O211]-SP≫ senktide, indicating binding to NK-2 receptors. Preliminary studies demostrated high specific binding in membranes from rat urinary bladder, duodenum and colon. Specific binding in rat brain and lung was negligible, and binding in a range of guinea-pig tissues was no more than 35% specific. These data may indicate species differences in NK-2 receptors.",

keywords = "Neuropeptide γ, NK-2 receptor, Rat gastric fundus, Selective radioligand, Tachykinin",

author = "Tim Badgery-Parker and Xiang-Ping Zeng and Solange Lavielle and Elizabeth Burcher",

year = "1993",

month = jul,

day = "2",

doi = "10.1016/0167-0115(93)90118-R",

language = "English",

volume = "46",

pages = "455--457",

journal = "Regulatory Peptides",

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T1 - A novel, selective radioligand, [125I]-[Lys5, Tyr(I2)7, Meleu9, Nle10]-NKA(4-10), for the tachykinin NK-2 receptor

AU - Badgery-Parker, Tim

AU - Zeng, Xiang-Ping

AU - Lavielle, Solange

AU - Burcher, Elizabeth

PY - 1993/7/2

Y1 - 1993/7/2

N2 - A new radioligand, [125I]-[Lys5Tyr(I2)7,MeLeu9,Nle10]-NKA(4-10), based on the selective agonist [Lys5,MeLeu9,Nle10]-NKA(4-10) has been developed. Binding in rat fundus membranes was displaced by NPγ>NKA≥[Lys5,MeLeu9,Nle10]-NKA(4-10)>neuropeptide K> Lys5,Tyr I2MeLeu9,Nle10]-NKA(4-10)>SP> [Sar9,Met(O211]-SP≫ senktide, indicating binding to NK-2 receptors. Preliminary studies demostrated high specific binding in membranes from rat urinary bladder, duodenum and colon. Specific binding in rat brain and lung was negligible, and binding in a range of guinea-pig tissues was no more than 35% specific. These data may indicate species differences in NK-2 receptors.

AB - A new radioligand, [125I]-[Lys5Tyr(I2)7,MeLeu9,Nle10]-NKA(4-10), based on the selective agonist [Lys5,MeLeu9,Nle10]-NKA(4-10) has been developed. Binding in rat fundus membranes was displaced by NPγ>NKA≥[Lys5,MeLeu9,Nle10]-NKA(4-10)>neuropeptide K> Lys5,Tyr I2MeLeu9,Nle10]-NKA(4-10)>SP> [Sar9,Met(O211]-SP≫ senktide, indicating binding to NK-2 receptors. Preliminary studies demostrated high specific binding in membranes from rat urinary bladder, duodenum and colon. Specific binding in rat brain and lung was negligible, and binding in a range of guinea-pig tissues was no more than 35% specific. These data may indicate species differences in NK-2 receptors.

KW - Neuropeptide γ

KW - NK-2 receptor

KW - Rat gastric fundus

KW - Selective radioligand

KW - Tachykinin

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U2 - 10.1016/0167-0115(93)90118-R

DO - 10.1016/0167-0115(93)90118-R

M3 - Article

C2 - 8210504

AN - SCOPUS:0027248783

SN - 0167-0115

VL - 46

SP - 455

EP - 457

JO - Regulatory Peptides

JF - Regulatory Peptides

IS - 1-2

ER -

A novel, selective radioligand, [¹²⁵I]-[Lys⁵, Tyr(I₂)⁷, Meleu⁹, Nle¹⁰]-NKA(4-10), for the tachykinin NK-2 receptor

Abstract

Keywords

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