(Leu sup 9. phi. (CH sub 2 NH)Leu sup 10 )-neurokinin A(4-10) (MDL 28,564) distinguishes tissue tachykinin peptide NK sub 2 receptors

Journal Article · Mon Jan 01 04:00:00 EST 1990 · Life Sciences; (USA)

OSTI ID:6159442

Buck, S H; Harbeson, S L; Hassmann, III, C F; Shatzer, S A ^[1]; Rouissi, N; Nantel, F ^[2]; van Giersbergen, P L.M. ^[3]

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1. Merrell Dow Research Institute, Cincinnati, OH (USA)
2. Univ. of Sherbrooke, Quebec (Canada)
3. Merrell Dow Research Institute, Cincinnati, OH (USA) Univ. of Cincinnati, OH (USA)

The neurokinin A analogue, MDL 28,564 (Asp-Ser-Phe-Val-Gly-Leu-CH{sub 2}NH-Leu-NH{sub 2}), inhibited {sup 125}I-NKA binding to hamster urinary bladder NK{sub 2} receptors with a K{sub I} of 130 nM. For rat submaxillary gland NK{sub 1} receptors and cerebral cortical NK{sub 3} receptors, the K{sub I}'s for MDL 28,564 were >250 {mu}M and >500 {mu}M, respectively. MDL 28,564 did not relax dog carotid artery (NK{sub 1} tissue) or contract rat portal vein (NK{sub 3} tissue). In guinea pig trachea tissues, MDL 28,564 stimulated phosphatidylinositol turnover and induced contraction with maximum effects similar to those of neurokinin A. In hamster urinary bladder tissue, MDL 28,564 stimulated phosphatidylinositol turnover with maximum effect only 10% of that of neurokinin A, did not produce sustained contraction itself and antagonized NKA-induced contraction. MDL 28,564 also produced full contraction in rabbit pulmonary artery (NK{sub 2} tissue) but was inactive in rat vas deferens (NK{sub 2} tissue). These data with MDL 28,564 are consistent with the NK{sub 2} receptors in guinea pig trachea and rabbit pulmonary artery being different form those in hamster urinary bladder and rat vas deferens.

• OSTI ID: 6159442
• Journal Information: Life Sciences; (USA), Journal Name: Life Sciences; (USA) Vol. 47:10; ISSN 0024-3205; ISSN LIFSA
• Country of Publication: United States
• Language: English

Related Subjects

550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
ANIMALS
ARTERIES
BETA DECAY RADIOISOTOPES
BIOCHEMICAL REACTION KINETICS
BLADDER
BLOOD VESSELS
BODY
CARDIOVASCULAR SYSTEM
CAROTID ARTERIES
DAYS LIVING RADIOISOTOPES
DOGS
ELECTRON CAPTURE RADIOISOTOPES
ESTERS
GUINEA PIGS
HAMSTERS
INHIBITION
INTERMEDIATE MASS NUCLEI
IODINE 125
IODINE ISOTOPES
ISOTOPE APPLICATIONS
ISOTOPES
KINETICS
KININS
LIPIDS
MAMMALS
MEMBRANE PROTEINS
NUCLEI
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANIC PHOSPHORUS COMPOUNDS
ORGANS
PEPTIDES
PHOSPHOLIPIDS
POLYPEPTIDES
PROTEINS
RABBITS
RADIOISOTOPES
RADIORECEPTOR ASSAY
RATS
REACTION KINETICS
RECEPTORS
RODENTS
TRACER TECHNIQUES
URINARY TRACT
VERTEBRATES