Ketanserin

Ketanserin (25) is an antihypertensive agent acting as an antagonist at both the serotonin-S2 and Qj-adrencrgic receptors [22]. Bendroflumethiazide (26) is the most notable in a class of diuretic-antihypertensive agents [5]... 

Cj H7N 140-29-4) see Azatadine Dicycloverine Disopyramide Ethoheptazine Isoaminile Levocabastine Mephenytoin Methylphenidate Methylphenobarbital Milnacipran hydrochloride Oxeladin Pentapiperide Pentoxyverine Pethidine Phenglutarimide Pheniramine Phenobarbital Tolazoline Triamterene Valethamate bromide 1 -benzy l-4-cyanopiperidine (C]3H 9N2 62778-37-4) see Ketanserin... 

C2H7NO 141-43-5) see Alibendol Butethamine Ciclopirox Cloxazolam Flomoxef Haloxazolam loxitalamic acid Ketanserin Levamisole Lomustine Mabuprofen Miltefosine Nicorandil Oxetacaine Phenoxybenzamine Piperazine... 

However, the specific serotonin uptake inhibitor fluoxetine failed to produce an MBDB-like cue and failed to block the stimulus effects of MBDB when it was given prior to a training dose of MBDB. Table 3 summarizes results of fluoxetine testing in MBDB-trained rats. In other exploratory studies, pretreatment of MDMA-trained rats with either methysergide or ketanserin failed to block completely the MDMA-discriminative stimulus. 

ANSWER We have tried ketanserin, but it did not antagonize the stimulus. I do not believe we have tested fluoxetine in the MBDB-trained animals. It has only been tested in the MDMA-trained animals. We have not found an antagonist to the cue yet. 

Ki values and Hill coefficents determined by competition experiments for 1.0 nM [ H]LSD(+[10- M]Ketanserin)-labeled sites in rat frontal cortical homogenates. Data from Shannon et al. 1984. 

FIGURE 3. Competition curves of (A) serotonin and (B) MDMA for fH] ketanserin binding to 5-HT serotonin receptors in rat frontal cortex membranes in the presence and absence of the guanine nucleotide quanosine-5-triphosphate (GTP)... 

Kirov, R. Moyanova, S. (1998a). Age-dependent effect of ketanserin on the sleepwaking phases in rats. Int.J. Neurosci 93, 257-64. 

The question as to where the common 5-HT and/or hallucinogen receptor is located is an intriguing one that cannot be answered convincingly at present. An important lead to its eventual characterization comes from the work of Leysen and Tollenaere (51) and Colpaert et al. (22), who describe two selective 5-HT/LSD antagonists, pirenperone and ketanserin. Investigators in our laboratories have confirmed the specificity of these compounds and observed an... 

Compounds S, binding hippocampus (3H-5-HT) (Ki = nM) S2 binding frontal cortex (3H-ketanserin) (K = nM)... 

The ligand hippocampal binding was 3H-5-HT and in the frontal cortex was 3H-ketanserin. Competitors were studied in the presence of each radioactive ligand and individual K, values determined. (Data reproduced from ref. 51.)... 

---