The lack of utility of the rat vas deferens as a functional bioassay for sigma ligands

The present study examined the utility of the rat vas deferens preparation as a bioassay for sigma site ligands. sigma Ligands such as (+/-)-pentazocine, phencyclidine (PCP) and (+)-SK&F 10047 potentiated neurogenic twitch contractions. However, neither the order of potency nor the absolute pote...

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Published inEuropean journal of pharmacology Vol. 193; no. 2; p. 139
Main Authors Fox, P K, Connick, J H, Hanlon, G M, France, L, Nicholson, C D
Format Journal Article
LanguageEnglish
Published Netherlands 07.02.1991
Subjects
Animals
Binding Sites
Biological Assay
Electric Stimulation
Guanidines - pharmacology
Guinea Pigs
Haloperidol - pharmacology
Male
Muscle Contraction - drug effects
Pentazocine - pharmacology
Phenazocine - analogs & derivatives
Phenazocine - pharmacology
Phencyclidine - pharmacology
Rats
Rats, Inbred Strains
Vas Deferens - drug effects
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Summary:The present study examined the utility of the rat vas deferens preparation as a bioassay for sigma site ligands. sigma Ligands such as (+/-)-pentazocine, phencyclidine (PCP) and (+)-SK&F 10047 potentiated neurogenic twitch contractions. However, neither the order of potency nor the absolute potency of (+/-)-pentazocine and (+)-SK&F 10047 correlated with their affinity at central sigma sites. Furthermore, another potent sigma ligand, ditolyl-ortho guanidine (DTG) neither affected neurogenic twitch contractions nor inhibited twitch potentiation by PCP or (+)-SK&F 10047 at concentrations up to 30 mumol/l. These data indicate that the rat vas deferens is not a useful bioassay for the evaluation of sigma ligands. PCP, (+)-SK&F 10047 and (+/-)-pentazocine probably enhance neurogenic contractions in rat vas deferens primarily by inhibition of the neuronal uptake of noradrenaline.
ISSN:0014-2999
DOI:10.1016/0014-2999(91)90028-O