5-HT2A receptor inverse agonists(Serotonin 2a (5-HT2a) receptor inverse agonists), 5-HT2B receptor inverse agonists(Serotonin 2b (5-HT2b) receptor inverse agonists), 5-HT2C receptor inverse agonists(Serotonin 2c (5-HT2c) receptor inverse agonists)

+ [3]

Therapeutic Areas

Other Diseases

Active Indication-

Inactive Indication

Behavioural disorders

Originator Organization

H. Lundbeck A/S

Active Organization-

Inactive Organization

H. Lundbeck A/S

Drug Highest PhasePendingPhase 1

First Approval Date-

Regulation-

Structure

Molecular FormulaC22H24F4N2O

InChIKeyJSBWGXQXCRYYTG-LMPOMZQGSA-N

CAS Registry80273-79-6

100 Clinical Results associated with Tefludazine

100 Translational Medicine associated with Tefludazine

100 Patents (Medical) associated with Tefludazine

Literatures (Medical) associated with Tefludazine

01 Oct 2001·Journal of Molecular Graphics and ModellingQ4 · BIOLOGY

Molecular field analysis of clozapine analogs in the development of a pharmacophore model of antipsychotic drug action

Q4 · BIOLOGY

Article

Author: Benjamin G. Tehan ; Edward J. Lloyd ; Margaret G. Wong

In an attempt to elucidate some aspects of clozapine's favorable receptor binding profile, we modeled a series of 30 clozapine analogs using a pharmacophore based on the ligands octoclothepin and tefludazine. Molecular field analysis using CoMFA combined with HINT was carried out on published D2 receptor binding affinities. Several alternative alignments of the analogs gave r2 values in the range of 0.8-0.95. The final model had good predictive abilities with q2 > 0.6 and r2 > 0.9. This provides an excellent framework to aid in the design of novel antipsychotics with diminished propensity to produce clinically limiting side effects.

01 Mar 1993·PsychopharmacologyQ3 · MEDICINE

Serotonergic and dopaminergic aspects of neuroleptic-induced extrapyramidal syndromes in nonhuman primates

Q3 · MEDICINE

Article

Author: Casey, D E

Neuroleptic drug-induced acute extra-pyramidal syndromes are one of the major reasons why patients discontinue their antipsychotic medicines. The typical (e.g., haloperidol) neuroleptic drug produces acute extrapyramidal symptoms in the majority of patients, whereas the atypical (clozapine) neuroleptic produces only minimal motor system side effects. Serotonin S2 antagonists often reduce or prevent catalepsy in rodents, but the limited number of studies in nonhuman primates have produced conflicting results. The hypothesis of a high serotonin S2/dopamine D2 antagonism ratio as a mechanism underlying atypical neuroleptic effects in preventing acute extrapyramidal syndromes deserves further evaluation in nonhuman primate models because extrapyramidal symptoms in monkeys closely resemble those in patients. Cebus monkeys (22-28 years old) were tested with compounds that ranged from low to high S2/D2 antagonism ratios. These were haloperidol, fluphenazine, clopenthixol, melperone, tefludazine, setoperone, risperidone, and clozapine. A saline control was included with a wide dose range of each of these drugs that was tested in a once-weekly, blindly-scored random drug administration schedule. Dystonia was scored on four different symptoms by an experienced rater who was blind to drug dosage. All the compounds, with the exception of clozapine, produced clinically indistinguishable dose-related dystonia. The only difference was the dose at which dystonia appeared. In contrast to rodent studies, these nonhuman primate investigations with drugs, spanning a wide range of S2/D2 antagonism ratios, produced clinically similar extrapyramidal symptoms. Thus, adding an S2 antagonism component to neuroleptics does not appear to provide an explanation for the motor side effect profile of atypical neuroleptics, or a method for designing neuroleptic drugs that will be free of extrapyramidal symptoms.

01 Jan 1989·Psychopharmacology bulletin

Serotonergic aspects of acute extrapyramidal syndromes in nonhuman primates.

Article

Author: Casey, D E

Neuroleptic drug-induced acute extrapyramidal syndromes (EPS) are the major reasons why patients discontinue their antipsychotic medicines. Serotonin S2 antagonists prevent catalepsy in rodents but the effects in nonhuman primates have received only minimal study and deserve further evaluation as potential "non-neuroleptic neuroleptics" (antipsychotic effects free of acute EPS). Twenty Cebus monkeys (22 to 28 yrs. old) were tested with compounds that ranged from high to very low D2/S2 ratios. These were haloperidol, clopenthixol, tefludazine, and setoperone, all tested in the dosage range of .01 to .25 mg/kg and compared with saline i.m. once weekly in a random schedule. Dystonia was scored on four different symptoms by an experienced rater blind to drug dosage. All four active compounds produced clinically indistinguishable, dose related dystonia with very similar dose thresholds. In contrast to rodent studies these nonhuman primate investigations with drugs of widely differing D2/S2 antagonism ratios produced clinically similar EPS. Thus adding an S2 antagonism component to neuroleptics appears not to provide a unique approach to neuroleptic therapy which will be free of acute EPS.

100 Deals associated with Tefludazine

R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
Behavioural disorders	Phase 2	-	H. Lundbeck A/S	-

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