Antiserotonin activity

Cyproheptadine (Periactin, etc) 4 mg + Moderate sedation also has antiserotonin activity... 

T-Antiserotonin activity of aminofuran derivatives (32a, 33a) is lower than those of indole derivatives (32b, 33b).84... 

Methylation at the indole nitrogen group specifically enhances the serotonin antagonism exhibited by all ergot alkaloids. For example, 1-methyl-LSD and l-methyl-2-bromo-LSD exhibit antiserotonin activity several times greater than that of their nonmethylated parent compounds. 

Methoxy-cyproheptadine (-) -3-Methoxy-cyproheptadine anticholinergic activity (-1- )-3-Methoxy-cyproheptadine antiserotonin activity Remy et... 

The substituted imidazo-thiazole, dexamisole, has antidepressant properties and its isomer, levamisole, possesses anthelmintic and immunostimulant properties. Enantiomers of HA-966 (3-amino-l-hydroxypyrrolid-2-one) exhibit distinct central nervous system effects (+)-HA-966 is a selective glycine/A-methyl-o-aspartate receptor antagonist, but (-)-HA-966 is a potent i-butyrolactone-Uke sedative." A comparison of (+) and (-)-3-methoxycypro-heptadine shows that aU of the anticholinergic activity of the ( )-3-methoxycyproheptadine resides solely in the dextrorotatory enantiomer, while the antiserotonin activity resides in the levorotatory enantiomer." ... 

First-generation piperidines (cyproheptadine, phenin-damine) Cyproheptadine uniquely has both antihistamine and antiserotonin activity. Cyproheptadine and phenin-damine cause drowsiness and also have significant anticholinergic effects. 

Fluperlapine shows potent central antiserotonin activity [622]. The pharmacological profile is similar to that of clozapine with additional antidepressant properties [623]. It has a good antipsychotic effect and alleviated the apathetic and depressive syndromes in a trial with schizophrenic patients [624,625]. The drug is beneficial in the treatment of patients vulnerable to neurological side-effects [626]. 

Many new phenylpiperazine derivatives with combined neurological and hypotensive properties have been described5 54 gf these, AP 1161 (24), a CNS depressant with weaker adrenolytic action than chlorpromazine but stronger antiserotonin activity has been recommended for clinical trial as a psychotropic drug ... 

Chernikov MV, Vassiliev PM (2006) Computer screening for novel benzimidazole derivatives with a high 5-HT3-antiserotonin activity using information technology Microcosm. Bull Volgogr Res Cent RAMS 2 7-8... 

Vassiliev PM, Spasov AA, Maltsev DV et al (2013) In silico consensus search for condensed azole derivatives with a high 5-HT2A-antiserotonin activity. In Proceedings of the XX Jubilee Russian national congress Man and drug , Moscow, 15-19 Apr 2013, p 307... 

In Table 3 are reported the results of a study on the antihistamine and antiserotonin activity of cyproheptadine and cyproheptadine-10,11-epoxide (35). A comparison of the inhibitory activity of the two drugs was carried out on the enhanced vascular permeability induced by serotonin (5HT) or histamine (H) injected intradermally in rats. The antagonistic activity was expressed as percent inhibition of the amount of Evans blue, previously injected intravenously, that was found in the skin of treated animals as compared to control animals. The antiserotonin and antihistamine activity of cyproheptadine-10,11-epoxide did not differ from that of cyproheptadine. Also, there was no difference between the inhibition measured 30 minutes or 2 hours after the administration of the compounds. These epoxides seem therefore to have pharmacological importance since they may contribute to the total pharmacological activity of their parent compounds. 

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