Reduced number of alpha- and beta-adrenergic receptors in the myocardium of rats exposed to tobacco smoke.

The concentration of alpha- and beta-adrenergic receptors--as measured by specific [3H]WB-4101 and (-)-[3H]dihydroalprenolol binding--was diminished by 60% below control values in the hearts of rats exposed to tobacco smoke. These changes in receptor numbers took place almost immediately after tobacco smoke exposure and were rapidly reversible after termination of the exposure. The dissociation constant, KD, for [3H]WB-4101 was identical in exposed (KD = 0.34 +/- 0.09 nM) and control (KD = 0.35 +/- 0.07 nM) hearts but was significantly different in the case of (-)-[3H]dihydroalprenolol binding (exposed, KD = 2.83 +/- 0.30 mM vs. control KD = 5.22 +/- 0.61 nM). For beta-receptor binding there was no significant difference between exposed and control animals in the Ki values for (-)-epinephrine, (-)-norepinephrine, (-)-alprenolol, (+/-)-propranolol or timolol. (-)-Isoproterenol, however, was found to bind with lower affinity in exposed compared with control hearts. For alpha-receptor binding there was no significant difference between control and 'smoked' animals in the Ki values for (-)-epinephrine, (-0)-norepinephrine or phentolamine. The decrease in alpha- and beta-adrenergic receptor concentration may be related to the phenomenon of receptor desensitization resulting from a release of catecholamines in rats exposed to tobacco smoke.