Indoleamine antagonists: relative potencies as inhibitors of tryptamine- and 5-hydroxytryptophan-evoked responses. 1974

B V Clineschmidt, and V J Lotti

Four indoleamine antagonists were evaluated for relative potencies as inhibitors of tryptamine-induced forepaw clonus and 5-hydroxytryptophan-evoked head twitches. Methergoline was approximately three times more potent against the forepaw clonus than the head twitch response, whereas methysergide exhibited nearly equal activity in both tests. Cyproheptadine and cinanserin showed a profile opposite to methergoline and a greater degree of selectivity, being 25 to 40 times more potent as inhibitors of the 5-hydroxytryptophan- than of the tryptamine-induced response. These findings clearly demonstrate that the rank order of potency of indoleamine antagonists varies greatly depending upon the test procedure employed.

UI MeSH Term Description Entries
D008784 Methysergide An ergot derivative that is a congener of LYSERGIC ACID DIETHYLAMIDE. It antagonizes the effects of serotonin in blood vessels and gastrointestinal smooth muscle, but has few of the properties of other ergot alkaloids. Methysergide is used prophylactically in migraine and other vascular headaches and to antagonize serotonin in the carcinoid syndrome. Dimethylergometrin,Methylmethylergonovine,Deseril,Desril,Désernil-Sandoz,Methysergide Dimaleate,Methysergide Maleate,Sansert,UML-491,Dimaleate, Methysergide,Désernil Sandoz,Maleate, Methysergide,UML 491,UML491
D009207 Myoclonus Involuntary shock-like contractions, irregular in rhythm and amplitude, followed by relaxation, of a muscle or a group of muscles. This condition may be a feature of some CENTRAL NERVOUS SYSTEM DISEASES; (e.g., EPILEPSY, MYOCLONIC). Nocturnal myoclonus is the principal feature of the NOCTURNAL MYOCLONUS SYNDROME. (From Adams et al., Principles of Neurology, 6th ed, pp102-3). Myoclonus, Action,Myoclonus, Nocturnal,Myoclonus, Palatal,Polymyoclonus,Myoclonic Jerk,Myoclonic Jerking,Myoclonus Simplex,Myoclonus, Eyelid,Myoclonus, Intention,Myoclonus, Lower Extremity,Myoclonus, Oculopalatal,Myoclonus, Segmental,Myoclonus, Sleep,Myoclonus, Upper Extremity,Action Myoclonus,Extremity Myoclonus, Lower,Extremity Myoclonus, Upper,Eyelid Myoclonus,Intention Myoclonus,Jerk, Myoclonic,Jerking, Myoclonic,Jerks, Myoclonic,Lower Extremity Myoclonus,Myoclonic Jerks,Nocturnal Myoclonus,Oculopalatal Myoclonus,Palatal Myoclonus,Segmental Myoclonus,Simplex, Myoclonus,Sleep Myoclonus,Upper Extremity Myoclonus
D002934 Cinnamates Derivatives of cinnamic acid (the structural formula: phenyl-HC Cinnamate
D003533 Cyproheptadine A serotonin antagonist and a histamine H1 blocker used as antipruritic, appetite stimulant, antiallergic, and for the post-gastrectomy dumping syndrome, etc. Antergan,Dihexazin,Periactin,Peritol,Viternum
D004873 Ergolines A series of structurally-related alkaloids that contain the ergoline backbone structure. Ergoline
D005260 Female Females
D005528 Foot The distal extremity of the leg in vertebrates, consisting of the tarsus (ANKLE); METATARSUS; phalanges; and the soft tissues surrounding these bones. Feet
D006257 Head The upper part of the human body, or the front or upper part of the body of an animal, typically separated from the rest of the body by a neck, and containing the brain, mouth, and sense organs. Heads
D006916 5-Hydroxytryptophan The immediate precursor in the biosynthesis of SEROTONIN from tryptophan. It is used as an antiepileptic and antidepressant. 5-HTP,Hydroxytryptophan,Oxitriptan,Oxytryptophan,Tryptophan, 5-Hydroxy-,5 Hydroxytryptophan,5-Hydroxy- Tryptophan,Tryptophan, 5 Hydroxy
D000813 Anilides Any aromatic amide obtained by acylation of aniline.

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