The alteration of cardiac beta-adrenoceptor (beta-AR) and subtypes in Wistar rats of 48 and 10 weeks old were investigated by radioligand binding assay and functional determination of isolated perfused left atria. The results indicated that: (1) The density of cardiac total beta-AR was downregulated about 28% in 48 weeks old rats as compared with rats of 10 weeks old for both beta 1- and beta 2-AR; (2) The sensitivity of beta-AR and subtypes to isoproterenol in isolated perfused atria was significantly lowered in rats of 48 weeks old; (3) The beta-AR mediated contractile effect of 10 weeks old rat hearts was mainly attributed to beta 1 type, but equally to both beta 1 and beta 2 types in 48 weeks old rat hearts; (4) The two receptor subtypes showed mutually potentiation effect in 10 weeks old rat hearts when stimulated simultaneously, but only additive in 48 weeks old rat hearts.