Um. Parkkisenniemi et al., The endothelin ETB receptor agonist [I-125]BQ-3020 binds predominantly to nerves in the bovine retractor penis muscle and penile artery, PHARM TOX, 87(5), 2000, pp. 234-241
Preliminary pharmacological experiments have suggested that in the bovine r
etractor penis muscle there are relaxation-mediating endothelin ETB recepto
rs, at least part of which are located on the inhibitory nitrergic nerves.
The present work was undertaken to test this hypothesis by means of recepto
r autoradiography and additional pharmacological experiments. In the retrac
tor penis muscle and the penile artery, specific binding of the ETB recepto
r-selective agonist [I-125]BQ-3020 took place predominantly to nerve trunks
and minor nerve branches. The situation was the same in the dorsal metatar
sal artery, that was included as a reference because of its different inner
vation. Throughout the nerves the silver grains were evenly distributed ove
r the nuclei of Schwann cells and the spaces between them. In the retractor
penis there was also a small amount of specific binding to smooth muscle.
No specific endothelial binding was observed in any of the tissues examined
. The pharmacological studies confirmed that the relaxation of the retracto
r penis muscle induced by the ETB receptor-selective agonist, sarafotoxin S
6c, is susceptible to tetrodotoxin as well as to inhibition of nitric oxide
synthase. The relaxation was also characterized by inconsistency, weakness
and tachyphylaxis. The electrical field stimulation-induced submaximal rel
axation of the retractor penis was unaffected by stimulation or blockade of
ETB receptors. The autoradiography suggests that in all the three bovine t
issues studied there are ETB receptors located on nerves independently of t
he type of efferent nerve. The pharmacological experiments do not support t
he concept that in the bovine retractor penis muscle neuronal ETB receptors
exert important immediate effects on the functioning of the penile erectio
n-mediating nitrergic nerves.