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. 2001 Apr;51(4):355-8.
doi: 10.1046/j.1365-2125.2001.01356.x.

Effects of nociceptin and endomorphin 1 on the electrically stimulated human vas deferens

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Effects of nociceptin and endomorphin 1 on the electrically stimulated human vas deferens

R Bigoni et al. Br J Clin Pharmacol. 2001 Apr.

Abstract

Aims: To examine the effects of nociceptin (NC) and endomorphin 1 (EM1) on electrical field stimulation (EFS)-induced contractions of the human vas deferens (hVD).

Methods: Concentration-response curves to NC and EM1 were constructed in the absence and in presence of peptidase inhibitors (PI). In some experiments a NC receptor antagonist, [Phe1psi(CH2-NH)Gly2]NC(1-13)NH2 [F/G], 10 microM) or naloxone (1 microM) were included.

Results: All data are mean(95%CI). In the presence of PI, NC inhibited twitches (Emax = 67(44,90)%; pEC50 = 7.28(6.95,7.61)). NC inhibition was sensitive to [F/G]. EM1 also inhibited twitches both in the absence (Emax = 82(73,91)% pEC50 = 7.07(6.92,7.22)) and presence (Emax = 83(76,90)%; pEC50 = 7.00(6.91, 7.09)) of PI. EM1 inhibition was sensitive to naloxone.

Conclusions: These data suggest that hVD express NC and opioid receptors that inhibit neurogenic contractions.

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Figures

Figure 1
Figure 1
Inhibitory effects of NC (a), mean±s.e. mean, (n = 6–9) and EM1 (b), mean±s.e. mean, (n = 11–16) in the absence and presence of peptidase inhibitors (PI) on electrically stimulated hVD. In panel (c) the effect of [F/G] (10 µm) and naloxone (1 µm) on the inhibitory effect of NC (▪) and EM1 (□) (both 1 µm) are shown. Data in (c) are from n ≥ 3 (mean±s.e. mean) except for naloxone vs NC where the mean of 2 determinations showing no inhibition are given.

References

    1. Calo′ G, Guerrini R, Rizzi A, et al. Pharmacology of nociceptin and its receptor: a novel therapeutic target. Br J Pharmacol. 2000;129:355–358. - PMC - PubMed
    1. Zadina JE, Hackler L, Ge LJ, Kastin AJ. A potent and selective endogenous agonist for the µ-opiate receptor. Nature. 1997;386:499–502. - PubMed
    1. Guerrini R, Calo′ G, Rizzi A, et al. Address and message sequences for the nociceptin receptor: a structure- activity study of nociceptin-(1–13) -peptide amide. J Med Chem. 1997;40:1789–1793. 10.1021/jm970011b. - DOI - PubMed
    1. Calo′ G, Guerrini R, Bigoni R, et al. Structure-activity study nociceptin (1–13) -NH2 N-terminal tetrapeptide discovery a nociceptin receptor antagonist. J Med Chem. 1998;41:3360–3366. 10.1021/jm970805q. - DOI - PubMed
    1. Jenkinson DH, Barnard EA, Hoyer D, Humphrey PPA, Leff P, Shankley NP. International Union of Pharmacology Commitee on receptor nomenclature and drug classification. XI Recommendations on terms and symbols in quantitative pharmacology. Pharmacol Rev. 1995;47:255–266. - PubMed

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