1 The contractile action of the dipeptide carnosine (b-alanyl-L-histidine), active as a Zn·carnosine complex (Zn·Carn), was investigated in isolated rings of rabbit saphenous vein (RSV) and was found to be antagonized by the H 1 antagonist mepyramine. 2 Mepyramine-sensitive, histamine-induced contractures in RSV, were smaller (73+0.1%) and less well sustained than carnosine-induced contractures. In the radioligand binding assay, the e ect of carnosine can be described as a function of Zn·Carn concentration with an apparent logIC 50 of 75.61. This value is consistent with that obtained from the functional studies on RSV. 7 Histamine-induced contractures have an indomethacine-sensitive component (27.2+8.3% of control response), not apparent with carnosine-induced contractures. 8 Like histamine, carnosine evoked an H 2 -mediated (cimetidine-sensitive) relaxation in the presence of mepyramine, but was less potent (10.8+3.1% residual tension at 10 mM carnosine compared with 13.4+7.5% at 0.1 mM histamine). 9 Carnosine, like mepyramine, can`reveal' the H 2 -mediated relaxation of histamine providing further evidence that carnosine binds at the H 1 receptor. 10 We conclude that carnosine can act at the smooth muscle H 1 -receptor to provoke vasoconstriction and that it also has the potential to act at H 1 -receptors in CNS.