physalaemin and phyllomedusin

The rat urinary bladder was examined as a model for studying tachykinin receptors. The order of potency, the maximal effect and the slope of the dose-response curve were examined with six tachykinins - substance P (SP), physalaemin, phyllomedusin, uperolein, eledoisin, kassinin - and several substance P fragments - SP-(2-11), SP-(3-11), SP-(4-11) and SP-(6-11). The tachykinin receptor on the rat urinary bladder was shown to bind preferentially tachykinins having a hydrophilic amino acid residue in position 5-6, as occurs with physalaemin, phyllomedusin, eledoisin and kassinin. The N-terminal of the tachykinins and in particular substance P is suggested to play a major role in regulating affinity, intrinsic activity and the slope of the dose-response curve. The tachykinins are thought to exert a direct action on smooth muscle. An accessory binding site associated with the tachykinin receptor on rat urinary bladder was also identified. This accessory site binds the N-terminal amino acids of the tachykinins as well as some alpha-adrenergic compounds (phentolamine, prazosin, noradrenaline or adrenaline in the presence of propranolol). When the accessory binding site is occupied by adrenergic compounds, the affinity of the tachykinins is markedly reduced. This observation is interpreted to mean that catecholamines may have a modulatory influence on tachykinin activity on the rat urinary bladder.

Topics: Animals; Autacoids; Eledoisin; Female; In Vitro Techniques; Kassinin; Muscle Contraction; Nerve Tissue Proteins; Neuropeptides; Oligopeptides; Peptide Fragments; Physalaemin; Rats; Receptors, Adrenergic, alpha; Substance P; Tachykinins; Urinary Bladder