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TACR2  -  tachykinin receptor 2

Canis lupus familiaris

Synonyms: NK-2R, SKR
 
 
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High impact information on Tacr2

  • Pretreatment of dogs with the NK-2 receptor antagonist, SR 48968 dose-dependently (1-10 mg/kg, p.o.) blocked the bronchoconstriction and respiratory responses to NKA challenge [1].
  • We studied the effects of the non-peptide NK-2 receptor antagonist SR48968 on canine colonic tone under resting conditions and after stimulation by the selective NK-2 receptor agonist [beta Ala8] neurokinin A-(4-10) [2].
  • In contrast, the selective NK2 receptor antagonist, R396 (10 microM) had no effect on the response to substance P [3].
  • A structure-activity study on neurokinin A and its C-terminal fragment NKA (4-10) has been performed in order to find selective agonists for the NK-2 receptor and identify chemical modifications suitable for protecting the peptides from degradation, while maintaining activity [4].
  • Local administration of the selective NK2 receptor agonist [beta-Ala8]-NKA-(4-10) depressed right atrial neuronal activity (27.3 +/- 6.4 to 14.7 +/- 3.8 impulses/min; P < 0. 05), whereas the selective NK3 receptor agonist senktide augmented such activity (18.9 +/- 6.4 to 53.1 +/- 12.0 impulses/min; P < 0.05) [5].
 

Analytical, diagnostic and therapeutic context of Tacr2

  • A variety of animal models have been used to profile activity of the tachykinins, particularly rodents and guinea pigs, but little information exists regarding methods to evaluate NK1- and NK2-receptor antagonist activity in dogs [6].

References

  1. Bronchoconstrictor and respiratory effects of neurokinin A in dogs. Sherwood, J.E., Mauser, P.J., Chapman, R.W. J. Pharmacol. Exp. Ther. (1997) [Pubmed]
  2. A selective NK-2 antagonist blocks the increase of canine colonic tone and ileal contractions induced by the NK-2 selective receptor agonist, [beta Ala8] neurokinin A-(4-10). Basilisco, G., Phillips, S.F. Aliment. Pharmacol. Ther. (1994) [Pubmed]
  3. Characterization of the receptor mediating relaxation to substance P in canine middle cerebral artery: no evidence for involvement of substance P in neurogenically mediated relaxation. Stubbs, C.M., Waldron, G.J., Connor, H.E., Feniuk, W. Br. J. Pharmacol. (1992) [Pubmed]
  4. Structure-activity studies of neurokinin A. Rovero, P., Pestellini, V., Rhaleb, N.E., Dion, S., Rouissi, N., Tousignant, C., Télémaque, S., Drapeau, G., Regoli, D. Neuropeptides (1989) [Pubmed]
  5. Canine intrinsic cardiac neurons involved in cardiac regulation possess NK1, NK2, and NK3 receptors. Thompson, G.W., Hoover, D.B., Ardell, J.L., Armour, J.A. Am. J. Physiol. (1998) [Pubmed]
  6. A method to measure dual NK1/NK2-antagonist activity in dogs. Sherwood, J.E., Young, S., Selig, W., Schilling, A., Kreutner, W., Egan, R.W., Chapman, R.W. Journal of pharmacological and toxicological methods. (1998) [Pubmed]
 
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