TY - JOUR
T1 - Characterization of flufylline, fluprofylline, ritanserin, butanserin and R 56413 with respect to in‐vivo α1‐, α2‐ and 5‐HT2‐receptor antagonism and in‐vitro affinity for α1‐, α2‐ and 5‐HT2‐receptors
T2 - comparison with ketanserin
AU - Korstanje, C.
AU - Sprenkels, R.
AU - Doods, H. N.
AU - Hugtenburg, J. G.
AU - Boddeke, E.
AU - Batink, H. D.
AU - Thoolen, M. J.M.C.
AU - Van Zwieten, P. A.
PY - 1986/1/1
Y1 - 1986/1/1
N2 - The experimental drugs butanserin (R 53393), ritanserin (R 55667), R 56413, flufylline (Sgd 195/78) and fluprofylline (Sgd 144/80) were evaluated with respect to their antagonism at postjunctional α1‐ and α2‐adrenoceptors and 5‐HT2‐receptors in pithed rats. Moreoever, affinity for [3H]mianserin, [3H]prazosin and [3H]yohimbine binding sites was assessed using rat brain preparations. In all experiments ketanserin was taken as a reference compound. It is concluded that of the compounds investigated butanserin is the most potent and selective α1‐adrenoceptor antagonist, whereas ritanserin was found to be a potent and selective 5‐HT2‐antagonist. Of the other compounds, fluprofylline was a very selective though not very potent α1‐adrenoceptor antagonist. The other compounds were less active and less selective in this respect.
AB - The experimental drugs butanserin (R 53393), ritanserin (R 55667), R 56413, flufylline (Sgd 195/78) and fluprofylline (Sgd 144/80) were evaluated with respect to their antagonism at postjunctional α1‐ and α2‐adrenoceptors and 5‐HT2‐receptors in pithed rats. Moreoever, affinity for [3H]mianserin, [3H]prazosin and [3H]yohimbine binding sites was assessed using rat brain preparations. In all experiments ketanserin was taken as a reference compound. It is concluded that of the compounds investigated butanserin is the most potent and selective α1‐adrenoceptor antagonist, whereas ritanserin was found to be a potent and selective 5‐HT2‐antagonist. Of the other compounds, fluprofylline was a very selective though not very potent α1‐adrenoceptor antagonist. The other compounds were less active and less selective in this respect.
UR - http://www.scopus.com/inward/record.url?scp=0022576736&partnerID=8YFLogxK
U2 - https://doi.org/10.1111/j.2042-7158.1986.tb04590.x
DO - https://doi.org/10.1111/j.2042-7158.1986.tb04590.x
M3 - Article
C2 - 2872314
SN - 0022-3573
VL - 38
SP - 374
EP - 379
JO - Journal of Pharmacy and Pharmacology
JF - Journal of Pharmacy and Pharmacology
IS - 5
ER -