Brady kinin

Figure 4.6. Log dose-response relationships for the effects of synthetic neurotensin, synthetic brady-kinin, and various preparations of NRP on the release of histamine from isolated rat mast cells [73], Each point is the mean obtained for two separate incubations.

An example of a pseudopeptide containing the CH2-NH group is afforded by N/t9,CH2-NH brady kinin. This analogue was stabilized not only against carboxypeptidase, which cleaves bradykinin at the 8,9-position, but also against ACE, which cleaves it at the 7,8-position (see Table 6.6). 

It has been suggested that y-turns are present in the solution structures of several peptides, and furthermore implicated in their bioactive conformations 101 including brady-kinin, 111 substance P,1121 cyclic somatostatin analogues, 131 cyclolinopeptide, 141 and the 6-opioid receptor bound conformation of enkephalin. 151 Yet, despite the fact that y-tums are frequently hypothesized to represent important features of secondary structure 161 based upon computational,1171 IR absorption,1181 NMR spectroscopic,119 201 and X-ray diffraction crystallographic determinations,1211 verification of the role of this predicted secondary structural element remains a difficult, but nonetheless critical step. 

This class of haptens includes those that have a carboxyl group, such as acetylsalicylic acid (aspirin) or the peptides angiotensin and brady-kinin. In addition, many haptens, such as some steroids, may have reactive groups to which a carboxyl group can be attached as, for example, by reaction with succinic anhydride (see below). For conjugation to proteins, the same procedures may be used regardless of whether the carboxyl group is present as an inherent part of the hapten or as an added moiety. 

Fig. 2 Gradient separation of peptide mixture on a C30 bonded phase. Mobile phase, linear gradient from 25% to 45% A in 15 min. A = 0.1% trifluoroacetic acid (TFA) in 75 25 acetonitrile-water and B = 0.1% TFA in water. Solutes 1 = brady-kinin 2 = angiotensin III 3 = angiotensin I.

Zabrocki, J., Dunbar, J. B. Jr., Marshall, K. W., Toth, M. V., and Marshall, G. R. (1992) Conformational mimicry. Part III. Synthesis and incorporation of 1,5-disubstituted tetrazole dipeptide analogs into peptides with preservation of chiral integrity Brady-kinin./. Org. Cbem. 57, 202-209. 

The effect of acetylcholine, dopamine, and brady-kinin on vascular tone has been examined in interlobular arteries and superficial afferent and efferent arterioles isolated from rabbit kidney [255]. AcetylchoUne caused a dose-dependent relaxation of norepinephrine-induced tone in all three vessel types. Significant relaxation was observed with 10(-8) M acetylcholine and higher concentrations caused complete relaxation. In afferent and efferent arterioles dopamine caused a dose-dependent relaxation that was indistinguishable... 

Wang C, Ford P, Chao C, Chao L, Chao J. Effect of cyclosporin A on the expression of tissue kallikrein, kininogen, and brady-kinin receptor in rat. Am J Physiol 1997 273 F783-F789. 

KoUarik M, Undem BJ (2004) Activation of bronchopulmonary vagal afferent nerves with brady-kinin, acid and vanilloid receptor agonists in wild-type and TRPVl-/- mice. J Physiol (Lond) 555 115-123... 

Figure 12. Proton decoupled C NMR spectrum of [90%-l,2- Ct Gly ] brady-kinin a, Full spectrum b. Carbonyl resonance c, Vpfield resonances. The Giy methylene resonances are doubled due to the slow cis/trans equilibrium with S cis-trans) = 1.1 ppm This effect is not observed for the carbonyl resonances for which S cis-transl = 0.0 ppm. (Reproduced from Ref. 63. Copyright 1982, American...

Yeo, W. W, I. Chadwick, M. Kraskiewicz, P. Jackson, and L. Ramsay. 1995. Resolution of ACE inhibitor cough Changes in subjective cough and responses to inhaled capsaicin, intradermal brady-kinin and substance-P. Br.). Clin. Pharmacol. 40(5) 423-429. 

Rat Uterus Kinin receptors Brady kinin / none 26... 

Brady kinin Bradykinin fragment Leucine encephalin... 

The production of three peptides, neokyrotiopin, VV-hemorphin-4, and brady-kinin-potentiating peptide, was monitored throughout the peptic hydrolysis of bovine hemoglobin using a 65-min 100/0- 33/67 (at 30 min)-> 23/87 wato- (0.1% TFA)/(60/40/0.1 acetonitrile/water/TFA) gradient. Peaks of interest were resolved and eluted in 30 min however, the elution of large peaks was seen imtil 60 min [1295],... 

Figure 23.20 CatA inhibition ieads to brady-kinin-dependent diuresis in rats. Anaesthetized rats received i.v. boius injections of compounds 10a, 12a, and 12b at I.Omg/kg (right side.) Urine was coiiected for the given...

As tachyphylaxis due to angiotensin can be prevented when the time between injections is sufficiently long in duration (14) or when the dissociation of the complex receptor - peptide is acdele-rated (20), it may be concluded that tachyphylaxis is due to resi-dually bound peptide. We therefore prefer the term auto-inhibition as the reduction of response is due to angiotensin itself and not to a persistent modification of muscular tissue. It must be noted that angiotensin tachyphylaxis on guinea-pig ileum is partially specific in that angiotensin renders the smooth muscle insensitive to itself but furthermore reduces its sensitivity to brady-kinin and in a lower extent to histamine in these conditions, action of acetylcholine is potentiated. 

The vasodilating action of caerulein and I.C.I. 50,123 on the pancreaticoduodenal vessels seems to be peculiar to these peptides only eledoisin, a peripheral vasodilating peptide, but not brady-kinin increased temporarily for 15-30 seconds the pancreaticoduode nal blood flow. This effect was followed promptly by a decrease in flow when blood pressure dropped. Similarly the hypotension caused by bradykinin was accompained by a corresponding decrease in blood flow. 

Figure 4. Histograms of output of acetylcholine from perfused cat submaxillary gland showing the effect of 1 ng and 10 ng of brady-kinin. Hatched bars represent acetylcholine released by electrical stimulation. White bars indicate the acetylcholine content of the control samples.

The chemical structures of bradykinin, kallidin and methionyl-lysyl-brady-kinin ( = methionyl-kallidin) are shown in Figure 6. 

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