In vivo pharmacology of [beta Ala8]neurokinin A-(4-10), a selective NK-2 tachykinin receptor agonist.

Abstract

We studied the effect of [beta Ala8]neurokinin A-(4-10), a newly developed selective NK-2 tachykinin receptor agonist, on various parameters in anaesthetized rats (blood pressure, urinary bladder motility, plasma extravasation) and guinea-pigs (salivation, increase of pulmonary insufflation pressure) as compared to the response produced by tachykinins. [beta Ala8]Neurokinin A-(4-10) was as active as, or more active than, neurokinin A (NKA) or NKA-(4-10) in producing rat bladder contraction or bronchospasm in guinea-pigs, two effects known to involve activation of NK-2 receptors. On the other hand, the synthetic peptide was weakly active, if active at all, in producing hypotension or plasma extravasation in the rat bladder as well as salivation in guinea-pigs, effects known to involve activation of NK-1 receptors. These findings provide evidence that [beta Ala8]NKA-(4-10) acts as a selective NK-2 agonist in vivo and that it can be used to explore the distribution and function of NK-2 receptors.

• Authors: C A Maggi, S Giuliani, L Ballati, P Rovero, L Abelli, S Manzini, A Giachetti, A Meli
• Journal: European journal of pharmacology (Eur J Pharmacol) Vol. 177 Issue 1-2 Pg. 81-6 (Feb 20 1990) ISSN: 0014-2999 [Print] Netherlands
• PMID: 2160369 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Blood Proteins
• Peptide Fragments
• Receptors, Neurokinin-2
• Receptors, Neurotransmitter
• neurokinin A (4-10), beta-Ala(8)-
• Neurokinin A
• neurokinin A(4-10)

Topics

• Anesthesia
• Animals
• Blood Pressure (drug effects)
• Blood Proteins (metabolism)
• Bronchi (drug effects)
• Guinea Pigs
• In Vitro Techniques
• Male
• Muscle Contraction (drug effects)
• Muscle, Smooth (metabolism)
• Neurokinin A (analogs & derivatives, pharmacology)
• Peptide Fragments (pharmacology)
• Rats
• Rats, Inbred Strains
• Receptors, Neurokinin-2
• Receptors, Neurotransmitter (drug effects, physiology)
• Salivation (drug effects)
• Urinary Bladder (drug effects)