Ld. Leake et M. Koubanakis, CENTRAL AND PERIPHERAL 5-HT RECEPTORS IN THE LEECH (HIRUDO-MEDICINALIS) REDEFINED, General pharmacology, 26(8), 1995, pp. 1709-1717
1. 5-Hydroxytryptamine (5-HT) receptors in the Retzius neurones (R cel
ls) and longitudinal body wall muscle strips of the leech H. medicinal
is were studied using a range of selective agonists developed for mamm
alian receptors. 2. All agonists induced hyperpolarisation of R cells:
the order of their potency was 5-HT > 5-CT > 2-Me 5HT > alpha-Me-5-HT
> > CGS-12066B = 5MeOT > PAPP > Buspirone. This receptor is most like
a mammalian 5-HT1C/2 receptor. 3. 5-HT induces relaxation of body wal
l strips, preceded at higher doses by contraction or an increase in sp
ontaneous contractions. The relaxing effect was best mimicked by 5-CT
and alpha-Me-5-HT, suggesting a 5-HT1C/2 receptor. The contractile eff
ect was best mimicked by 5-MeOT suggesting a 5-HT4-like receptor. The
overall potency of agonists on the body wall muscle was 5-MeOT > 5-CT
> 5-HT > alpha-Me-5-HT > 2-Me 5-HT > PAPP > Buspirone > > CGS-12066B.
4. Results suggest that either the sites of 5-HT action possess severa
l different receptors or the receptors themselves are more complex wit
h multiple properties.