F. Guirimand et al., EFFECTS OF INTRATHECAL AND INTRACEREBROVENTRICULAR BUPRENORPHINE ON AC-FIBER REFLEX IN THE RAT, The Journal of pharmacology and experimental therapeutics, 275(2), 1995, pp. 629-637
A C-fiber reflex elicited by electrical stimulation within the territo
ry of the ipsilateral sural nerve, was recorded from the biceps femori
s muscle in anesthetized rats. The temporal evolution of the reflex wa
s studied using a constant level of stimulus intensity (3 x threshold)
and recruitment curves were built by varying stimulus intensity from
0 to 7 x threshold. Intrathecal doses of buprenorphine in the 0.2 to 1
0 mu g range, elicited a facilitation of the C-fiber reflex in a dose-
dependent manner. A large dose (100 mu g) depressed but did not block
the reflex. Intracerebroventricular doses of buprenorphine in the 0.1
to 10 mu g range, facilitated the C-fiber reflex. A higher dose (100 m
u g) elicited a biphasic effect: depressive when the stimulus intensit
y was weak and facilitatory when the stimulus intensity was strong. It
is concluded that the antinociceptive properties of buprenorphine can
not be related to a direct or indirect depressive spinal effect. In te
rms of spinal and supraspinal effects of buprenorphine, it is likely t
hat buprenorphine facilitates the C-fiber reflex via a supraspinal mec
hanism that acts on sensory and/or motor components of the reflex are
although the depression of the reflex involves a spinal mechanism. The
lipophilic properties of buprenorphine could explain a substantial di
ffusion from its spinal injection site to the brain. From a clinical s
tandpoint, this study confirms that intrathecal administration of bupr
enorphine is an inadequate way of accessing spinal opioid receptors.