Characterisation of a novel, selective radioligand, [125I][Lys5,Tyr(I2)7,MeLeu 9,Nle10]neurokinin A-(4-10), for the tachykinin NK2 receptor in rat fundus

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

doi:10.1016/0014-2999(93)90051-I

Characterisation of a novel, selective radioligand, [¹²⁵I][Lys⁵,Tyr(I₂)⁷,MeLeu ⁹,Nle¹⁰]neurokinin A-(4-10), for the tachykinin NK₂ receptor in rat fundus

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

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

22 Citations (Scopus)

Abstract

The tyrosyl derivative of the tachykinin NK₂ selective agonist [Lys⁵,MeLeu⁹,Nle¹⁰]NKA-(4-10) was iodinated and the product [¹²⁵I][Lys⁵,Tyr(I₂)²,MeLeu ⁹,Nle¹⁰]NKA-(4-10) purified using reverse phase HPLC. The binding characteristics of this novel radioligand were investigated in homogenates of rat gastric fundus. Binding was saturable, reversible and to a single population of high affinity sites of K_D 1.3 ± 0.2 nM (n = 4). Specific binding of [¹²⁵I][Lys⁵,Tyr(I₂)⁷,MeLeu ⁹,Nle¹⁰ ]NKA-(4-10) was inhibited by neuropeptide γ SR 48968 ≥ neurokinin A (NKA) ≥ [Lys⁵,MeLeu⁹,Nle¹⁰]NKA-(4-10) > [Lys⁵,Tyr⁷,MeLeu⁹,Nle¹⁰]NKA- (4 -10) > neuropeptide K > [Lys⁵,Tyr(I₂)⁷,MeLeu⁹,Nle ¹⁰]NKA-(4-10) > MDL 29,913 > [¹²⁷I]-Bolton-Hunter-NKA > neurokinin B > substance P (SP) ≫ MEN 10207 > [Sar⁹,Met(O₂)¹¹]SP ≫ senktide, indicating binding to NK₂ receptors. NKA, [Lys⁵,MeLeu⁹,Nle¹⁰]NKA-(4-10) and [Lys⁵,Tyr(I₂)⁷,MeLeu⁹,Nle ¹⁰]NKA-(4minus;10) contracted the isolated fundus strip, with pD₂ values 7.9, 7.7 and 7.4, respectively. This novel, highly selective radioligand should prove useful in characterisation studies in peripheral tissues.

Original language	English
Pages (from-to)	201-207
Number of pages	7
Journal	European Journal of Pharmacology
Volume	233
Issue number	2-3
DOIs	https://doi.org/10.1016/0014-2999(93)90051-I
Publication status	Published - 23 Mar 1993
Externally published	Yes

Keywords

Gastric fundus (rat)
Neurokinin A
Neuropeptide γ
NK receptors
Radioligand binding
Tachykinin

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10.1016/0014-2999(93)90051-I

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@article{17e877c6afb5462abe9b8a9da7f7f541,

title = "Characterisation of a novel, selective radioligand, [125I][Lys5,Tyr(I2)7,MeLeu 9,Nle10]neurokinin A-(4-10), for the tachykinin NK2 receptor in rat fundus",

abstract = "The tyrosyl derivative of the tachykinin NK2 selective agonist [Lys5,MeLeu9,Nle10]NKA-(4-10) was iodinated and the product [125I][Lys5,Tyr(I2)2,MeLeu 9,Nle10]NKA-(4-10) purified using reverse phase HPLC. The binding characteristics of this novel radioligand were investigated in homogenates of rat gastric fundus. Binding was saturable, reversible and to a single population of high affinity sites of KD 1.3 ± 0.2 nM (n = 4). Specific binding of [125I][Lys5,Tyr(I2)7,MeLeu 9,Nle10 ]NKA-(4-10) was inhibited by neuropeptide γ SR 48968 ≥ neurokinin A (NKA) ≥ [Lys5,MeLeu9,Nle10]NKA-(4-10) > [Lys5,Tyr7,MeLeu9,Nle10]NKA- (4 -10) > neuropeptide K > [Lys5,Tyr(I2)7,MeLeu9,Nle 10]NKA-(4-10) > MDL 29,913 > [127I]-Bolton-Hunter-NKA > neurokinin B > substance P (SP) ≫ MEN 10207 > [Sar9,Met(O2)11]SP ≫ senktide, indicating binding to NK2 receptors. NKA, [Lys5,MeLeu9,Nle10]NKA-(4-10) and [Lys5,Tyr(I2)7,MeLeu9,Nle 10]NKA-(4minus;10) contracted the isolated fundus strip, with pD2 values 7.9, 7.7 and 7.4, respectively. This novel, highly selective radioligand should prove useful in characterisation studies in peripheral tissues.",

keywords = "Gastric fundus (rat), Neurokinin A, Neuropeptide γ, NK receptors, Radioligand binding, Tachykinin",

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

year = "1993",

month = mar,

day = "23",

doi = "10.1016/0014-2999(93)90051-I",

language = "English",

volume = "233",

pages = "201--207",

journal = "European Journal of Pharmacology",

issn = "0014-2999",

publisher = "Elsevier",

number = "2-3",

}

Characterisation of a novel, selective radioligand, [¹²⁵I][Lys⁵,Tyr(I₂)⁷,MeLeu ⁹,Nle¹⁰]neurokinin A-(4-10), for the tachykinin NK₂ receptor in rat fundus. / Burcher, Elizabeth; Badgery-Parker, Tim; Zeng, Xiang-Ping et al.
In: European Journal of Pharmacology, Vol. 233, No. 2-3, 23.03.1993, p. 201-207.

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

TY - JOUR

T1 - Characterisation of a novel, selective radioligand, [125I][Lys5,Tyr(I2)7,MeLeu 9,Nle10]neurokinin A-(4-10), for the tachykinin NK2 receptor in rat fundus

AU - Burcher, Elizabeth

AU - Badgery-Parker, Tim

AU - Zeng, Xiang-Ping

AU - Lavielle, Solange

PY - 1993/3/23

Y1 - 1993/3/23

N2 - The tyrosyl derivative of the tachykinin NK2 selective agonist [Lys5,MeLeu9,Nle10]NKA-(4-10) was iodinated and the product [125I][Lys5,Tyr(I2)2,MeLeu 9,Nle10]NKA-(4-10) purified using reverse phase HPLC. The binding characteristics of this novel radioligand were investigated in homogenates of rat gastric fundus. Binding was saturable, reversible and to a single population of high affinity sites of KD 1.3 ± 0.2 nM (n = 4). Specific binding of [125I][Lys5,Tyr(I2)7,MeLeu 9,Nle10 ]NKA-(4-10) was inhibited by neuropeptide γ SR 48968 ≥ neurokinin A (NKA) ≥ [Lys5,MeLeu9,Nle10]NKA-(4-10) > [Lys5,Tyr7,MeLeu9,Nle10]NKA- (4 -10) > neuropeptide K > [Lys5,Tyr(I2)7,MeLeu9,Nle 10]NKA-(4-10) > MDL 29,913 > [127I]-Bolton-Hunter-NKA > neurokinin B > substance P (SP) ≫ MEN 10207 > [Sar9,Met(O2)11]SP ≫ senktide, indicating binding to NK2 receptors. NKA, [Lys5,MeLeu9,Nle10]NKA-(4-10) and [Lys5,Tyr(I2)7,MeLeu9,Nle 10]NKA-(4minus;10) contracted the isolated fundus strip, with pD2 values 7.9, 7.7 and 7.4, respectively. This novel, highly selective radioligand should prove useful in characterisation studies in peripheral tissues.

AB - The tyrosyl derivative of the tachykinin NK2 selective agonist [Lys5,MeLeu9,Nle10]NKA-(4-10) was iodinated and the product [125I][Lys5,Tyr(I2)2,MeLeu 9,Nle10]NKA-(4-10) purified using reverse phase HPLC. The binding characteristics of this novel radioligand were investigated in homogenates of rat gastric fundus. Binding was saturable, reversible and to a single population of high affinity sites of KD 1.3 ± 0.2 nM (n = 4). Specific binding of [125I][Lys5,Tyr(I2)7,MeLeu 9,Nle10 ]NKA-(4-10) was inhibited by neuropeptide γ SR 48968 ≥ neurokinin A (NKA) ≥ [Lys5,MeLeu9,Nle10]NKA-(4-10) > [Lys5,Tyr7,MeLeu9,Nle10]NKA- (4 -10) > neuropeptide K > [Lys5,Tyr(I2)7,MeLeu9,Nle 10]NKA-(4-10) > MDL 29,913 > [127I]-Bolton-Hunter-NKA > neurokinin B > substance P (SP) ≫ MEN 10207 > [Sar9,Met(O2)11]SP ≫ senktide, indicating binding to NK2 receptors. NKA, [Lys5,MeLeu9,Nle10]NKA-(4-10) and [Lys5,Tyr(I2)7,MeLeu9,Nle 10]NKA-(4minus;10) contracted the isolated fundus strip, with pD2 values 7.9, 7.7 and 7.4, respectively. This novel, highly selective radioligand should prove useful in characterisation studies in peripheral tissues.

KW - Gastric fundus (rat)

KW - Neurokinin A

KW - Neuropeptide γ

KW - NK receptors

KW - Radioligand binding

KW - Tachykinin

UR - https://www.scopus.com/pages/publications/0027483135

U2 - 10.1016/0014-2999(93)90051-I

DO - 10.1016/0014-2999(93)90051-I

M3 - Article

C2 - 8385622

AN - SCOPUS:0027483135

SN - 0014-2999

VL - 233

SP - 201

EP - 207

JO - European Journal of Pharmacology

JF - European Journal of Pharmacology

IS - 2-3

ER -

Characterisation of a novel, selective radioligand, [¹²⁵I][Lys⁵,Tyr(I₂)⁷,MeLeu ⁹,Nle¹⁰]neurokinin A-(4-10), for the tachykinin NK₂ receptor in rat fundus

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Keywords

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