The regional brain uptake of 99mTc-N,N'-(1,2-ethylenediyl)bis-L-cysteine diethyl ester (99mTc-bicisate) measured by single photon emission computed tomography (SPECT) was compared with the regional CBF and CMRO2 measured by positron emission tomography in patients with cerebrovascular disease. Nine patients with the diagnosis of cerebral ischemic disorders (n = 7) or cerebral hemorrhage (n = 2) were studied. 99mTc-Bicisate brain uptake correlated with CBF and CMRO2. However, 99mTc-bicisate uptake did not reflect CBF in the single lesion showing luxury perfusion, which seemed to resemble a CMRO2 image. Though quantitative analysis showed the nonlinear correspondence of 99mTc-bicisate brain uptake with CBF and CMRO2, this correspondence could be corrected into a more linear relationship using a correction factor. 99mTc-Bicisate washout from the brain had no correlation to CBF and CMRO2. This diffuse decreasing washout rate was approximately 15% during the first hour after injection. By using the lipophilic fraction of arterial blood and a linearized correction of 99mTc-bicisate SPECT images, the feasibility of obtaining a factor-related CBF and CMRO2 was suggested from our data. These results suggested that 99mTc-bicisate had good characteristics for routine clinical use with SPECT to display the brain function in patients with neurological disorders.