Lesopitron

Lesopitron
Clinical data
Routes of; administration	Oral
ATC code	none;
Legal status
Legal status	In general: uncontrolled;
Identifiers
	IUPAC name 2-{4-[4-(4-chloro-1H-pyrazol-1-yl)butyl]piperazin-1-yl}pyrimidine;
CAS Number	132449-46-8;
PubChem CID	60813;
ChemSpider	54801;
UNII	H1CGM4755H;
CompTox Dashboard (EPA)	DTXSID40157587 ;
Chemical and physical data
Formula	C15H21ClN6
Molar mass	320.83 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES Clc1cn(nc1)CCCCN3CCN(c2ncccn2)CC3;

Lesopitron (E-4424) is a selective full agonist of the 5-HT_1A receptor which is structurally related to the azapirones.^[1] In 2001 it was under development by Esteve as an anxiolytic for the treatment of generalized anxiety disorder (GAD).^[2]^[3] It made it to phase II clinical trials but was apparently discontinued as no new information on lesopitron has surfaced since.^[2]^[3]

References

^ Haj-Dahmane S, Jolas T, Laporte AM, et al. (April 1994). "Interactions of lesopitron (E-4424) with central 5-HT1A receptors: in vitro and in vivo studies in the rat". European Journal of Pharmacology. 255 (1–3): 185–96. doi:10.1016/0014-2999(94)90097-3. PMID 8026543.
^ ^a ^b Micheli F (February 2001). "Lesopitron (Esteve)". IDrugs: The Investigational Drugs Journal. 4 (2): 218–24. PMID 16032484.
^ ^a ^b Fresquet A, Sust M, Lloret A, et al. (February 2000). "Efficacy and safety of lesopitron in outpatients with generalized anxiety disorder". The Annals of Pharmacotherapy. 34 (2): 147–53. doi:10.1345/aph.19041. PMID 10676820.

[pmid8026543-1] Haj-Dahmane S, Jolas T, Laporte AM, et al. (April 1994). "Interactions of lesopitron (E-4424) with central 5-HT1A receptors: in vitro and in vivo studies in the rat". European Journal of Pharmacology. 255 (1–3): 185–96. doi:10.1016/0014-2999(94)90097-3. PMID 8026543.

[pmid16032484-2] Micheli F (February 2001). "Lesopitron (Esteve)". IDrugs: The Investigational Drugs Journal. 4 (2): 218–24. PMID 16032484.

[pmid10676820-3] Fresquet A, Sust M, Lloret A, et al. (February 2000). "Efficacy and safety of lesopitron in outpatients with generalized anxiety disorder". The Annals of Pharmacotherapy. 34 (2): 147–53. doi:10.1345/aph.19041. PMID 10676820.

[1]

[2]

[3]

v t e Anxiolytics (N05B)
5-HT_1ARTooltip 5-HT1A receptor agonists	Buspirone Gepirone Tandospirone
GABA_ARTooltip GABAA receptor PAMsTooltip positive allosteric modulators	Benzodiazepines: Adinazolam Alprazolam Bromazepam Camazepam Chlordiazepoxide Clobazam Clonazepam Clorazepate Clotiazepam Cloxazolam Diazepam^# Ethyl loflazepate Etizolam Fludiazepam Halazepam Ketazolam Lorazepam^# Medazepam Nordazepam Oxazepam Pinazepam Prazepam; Others: Alpidem^‡ Barbiturates (e.g., phenobarbital) Carbamates (e.g., meprobamate) Carisoprodol Chlormezanone^‡ Ethanol (alcohol) Etifoxine
Hypnotics	Zopiclone
Gabapentinoids (α₂δ VDCC blockers)	Gabapentin Gabapentin enacarbil Phenibut Pregabalin
Antidepressants	SSRIsTooltip Selective serotonin reuptake inhibitors (e.g., escitalopram) SNRIsTooltip Serotonin-norepinephrine reuptake inhibitors (e.g., duloxetine) SARIsTooltip Serotonin antagonist and reuptake inhibitors (e.g., trazodone) TCAsTooltip Tricyclic antidepressants (e.g., clomipramine^#) TeCAsTooltip Tetracyclic antidepressants (e.g., mirtazapine) MAOIsTooltip Monoamine oxidase inhibitors (e.g., phenelzine); Others: Agomelatine Bupropion Tianeptine Vilazodone Vortioxetine
Antipsychotics	Quetiapine Flupentixol
Sympatholytics (Antiadrenergics)	Alpha-1 blockers (e.g., prazosin) Alpha-2 agonists (e.g., clonidine, dexmedetomidine, guanfacine) Beta blockers (e.g., propranolol)
Others	Benzoctamine Cycloserine Fabomotizole Hydroxyzine Lorpiprazole Mebicar Mepiprazole Nicotine Opipramol Oxaflozane^‡ Phenaglycodol Phenibut Picamilon Selank Tiagabine Tofisopam Validolum
^#WHO-EM ^‡Withdrawn from market Clinical trials: ^†Phase III ^§Never to phase III

See also

References