Heterogeneity of tachykinin NK-2 receptors in rabbit, guinea-pig and human smooth muscles.
Recent evidence indicates that the tachykinin NK-2 receptor is heterogenous (subtypes/species variants) and the existence of NK-2A (or 'non-classical') and NK-2B (or 'classical') forms of the NK-2 receptor in mammalian tissues has been proposed. In this study we have compared the affinities of 7 linear octa- and heptapeptide derivatives of neurokinin A (4-10) and that of two cyclic hexapeptides endowed with selective NK-2 receptor antagonist properties in 5 mammalian smooth muscle preparations previously characterized as expressing the NK-2A receptor subtype (rabbit pulmonary artery and bronchus, guinea-pig bronchus, human ileum and colon) and 2 preparations previously characterized as expressing the NK-2B receptor subtype (rat vas deferens and hamster trachea). The results of this comparative study reinforce the concept of two broad categories of preparations expressing pharmacologically distinguishable forms of the tachykinin NK-2 receptor and suggest the possibility of a further heterogeneity within the previously defined NK-2A receptor subtype.
Maggi
C A
CA
Department of Pharmacology, A. Menarini Pharmaceuticals, Florence, Italy.
Giuliani
S
S
Patacchini
R
R
Quartara
L
L
Rovero
P
P
Renzetti
A R
AR
Mizrahi
J
J
Giachetti
A
A
D000595:Amino Acid Sequence; D000818:Animals; D006168:Guinea Pigs; D006801:Humans; D008969:Molecular Sequence Data; D009130:Muscle, Smooth / Q000737:chemistry*; D015288:Neurokinin A / Q000378:metabolism*; D010446:Peptide Fragments / Q000378:metabolism*; D011817:Rabbits; D011869:Radioligand Assay; D017981:Receptors, Neurotransmitter / Q000032:analysis*; D018039:Receptors, Tachykinin; D015320:Tachykinins / Q000032:analysis*
D010446:Peptide Fragments; D017981:Receptors, Neurotransmitter; D018039:Receptors, Tachykinin; D015320:Tachykinins; D015288:Neurokinin A; C056408:neurokinin A(4-10)