TiPS receptor and ion channel nomenclature supplement 1994

Vasoconstrictor endothelin receptors characterized in human renal artery and vein in vitro

“…ET-1 and ET-2 are more potent than ET-3 at the ETA receptor whereas all three have equal affinity for the ETB receptors (Sakurai et al, 1992;Watson & Girdlestone, 1993). The endothelin receptors which mediate the pathophysiological effects of ET in the human kidney have not yet been defined; indeed the physiological role of the endothelins and their receptors in the kidney remains to be clarified.…”

Endothelin receptors in human coronary artery and aorta

“…The ETA subtype is believed to have higher affinity for ET-1, ET-2 and sarafotoxin 6b (S6b) compared to ET-3 whereas ETB has equal affinity for the ET-1, ET-2 and ET-3 isopeptides and S6b (Kloog & Sokolovsky, 1989;Sokolovsky, 1994;Watson & Girdlestone, 1995). Vasocon-striction is stimulated by the interaction of endothelin with ETA receptors on vascular smooth muscle (Sakurai et al, 1992).…”

The use of receptor desensitization to analyse CCKA and CCKB/gastrin receptors coupled to contraction in guinea‐pig stomach muscle

“…In contrast, CCK-8 concentration-effect curves obtained in a separate experiment with another set of PG curves, extended over approximately 5 log cycles, were asymmetrical about the midpoint location as judged-by-eye and could not be fitted by the logistic function ( [B] is the concentration of L-365260 and KB was taken from the pA2 value estimated from the interaction between L-365260 and PG (Figure 2b). Agonist activity in guinea-pig gallbladder PG and TG are potent agonists at CCKB/gastrin receptors but are less active at CCKA-receptors (see Watson & Girdlestone, 1994). These compounds were thus considered potentially useful tools to desensitize CCKB/gastrin receptors selectively in the stomach muscle.…”

“…Selective agonists and antagonists are required for the pharmacological characterization of new assays. The native hormone, cholecystokinin (CCK) and its C-terminal octapeptide fragment, CCK-8, are non-selective agonists at CCKAand CCKB/gastrin receptors while gastrin, pentagastrin (PG, tert-butyloxycarbonyl-p-Ala-Trp-Met-Asp-Phe-NH2) and tetragastrin (TG, tert-butyloxycarbonyl-Trp-Leu-Asp-Phe-NH2) behave as selective stimulants of CCKB/gastrin receptors (see Watson & Girdlestone, 1994). Devazepide has been classified ' Author for correspondence.…”