Pexacerfont

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Pexacerfont

Systematic (IUPAC) name
8-(6-methoxy-2-methylpyridin-3-yl)-2,7-dimethyl-N-[(1R)-1-methylpropyl]pyrazolo[1,5-a]-1,3,5-triazin-4-amine
Clinical data
Legal status	Uncontrolled
Routes	Oral
Identifiers
CAS number	459856-18-9
ATC code	None
PubChem	CID ?
UNII	LF1VBG4ZUK^Y
KEGG	D10022^Y
Chemical data
Formula	C₁₈H₂₄N₆O
Mol. mass	340.4 g/mol
Y (what is this?) (verify)

Pexacerfont (BMS-562,086) is a drug developed by Bristol-Myers Squibb which acts as a CRF-1 antagonist.

Corticotropin releasing factor (CRF), also known as Corticotropin releasing hormone, is an endogenous peptide hormone which is released in response to various triggers such as chronic stress. This then triggers the release of corticotropin (ACTH), another hormone which is involved in the physiological response to stress. Chronic release of CRF and ACTH is believed to be directly or indirectly involved in many of the harmful physiological effects of chronic stress, such as excessive glucocorticoid release, diabetes mellitus, osteoporosis, stomach ulcers, anxiety, depression, and development of high blood pressure and consequent cardiovascular problems.^[1]

Pexacerfont is a recently developed CRF-1 antagonist which is currently in clinical trials for the treatment of anxiety disorders,^[2] and has also been proposed to be useful for the treatment of depression and irritable bowel syndrome.^[3]

A recent multicenter, randomized, double-blind, placebo-controlled trial found that Pexacerfont (100 mg/day) did not separate from placebo on the primary outcome measure (the mean change from baseline to end point in the Hamilton Anxiety Scale score). ^[4] These results suggest that blockade of CRF-1 receptor may not be a feasible treatment for anxiety disorders in certain human populations.

References

↑ Zoumakis E, Rice KC, Gold PW, Chrousos GP. Potential uses of corticotropin-releasing hormone antagonists. Annals of the New York Academy of Sciences. 2006 Nov;1083:239-51.
↑ ClinicalTrials.gov: Study of Pexacerfont (BMS-562086) in the Treatment of Outpatients With Generalized Anxiety Disorder
↑ STATEMENT ON A NONPROPRIETARY NAME ADOPTED BY THE USAN COUNCIL
↑ Coric V, Feldman HH, Oren DA, Shekhar A, Pultz J, Dockens RC, Wu X, Gentile KA, Huang SP, Emison E, Delmonte T, D'Souza BB, Zimbroff DL, Grebb JA, Goddard AW, Stock EG (2010). Multicenter, randomized, double-blind, active comparator and placebo-controlled trial of a corticotropin-releasing factor receptor-1 antagonist in generalized anxiety disorder. Depress Anxiety. 27(5):417-25. PMID 20455246.

Antidepressants (N06A)

Specific reuptake inhibitors (RIs), enhancers (REs), and releasing agents (RAs)

Selective serotonin reuptake inhibitors (SSRIs)	Alaproclate Citalopram Escitalopram Femoxetine Fluoxetine^# Fluvoxamine Indalpine Ifoxetine Litoxetine Omiloxetine Panuramine Paroxetine Pirandamine Seproxetine Sertraline Zimelidine^‡

Serotonin–norepinephrine reuptake inhibitors (SNRIs)	Clovoxamine Desvenlafaxine Duloxetine Levomilnacipran Eclanamine Milnacipran Sibutramine Venlafaxine

Serotonin–norepinephrine–dopamine reuptake inhibitors (SNDRIs)	Adhyperforin Amitifadine Bicifadine Brasofensine BTS-74,398 Cocaine Diclofensine DOV-102,677 DOV-216,303 EXP-561 Fezolamine Hyperforin JNJ-7925476 NS-2359 PRC200-SS Pridefine SEP-225,289 SEP-227,162 Tesofensine

Norepinephrine reuptake inhibitors (NRIs)	Amedalin Atomoxetine/Tomoxetine Binedaline Ciclazindol Daledalin Edivoxetine Esreboxetine Lortalamine Maprotiline Mazindol Nisoxetine Reboxetine Talopram Talsupram Tandamine Viloxazine

Dopamine reuptake inhibitors (DRIs)	Medifoxamine Vanoxerine

Norepinephrine-dopamine reuptake inhibitors (NDRIs)	Amineptine Bupropion/Amfebutamone Cilobamine Manifaxine Methylphenidate Nomifensine Radafaxine Tametraline

Norepinephrine-dopamine releasing agents (NDRAs)	Amphetamine Befuraline Lisdexamfetamine Methamphetamine Phenethylamine Piberaline Tranylcypromine

Serotonin-norepinephrine-dopamine releasing agents (SNDRAs)	4-Methyl-αMT αET/Etryptamine αMT/Metryptamine

Selective serotonin reuptake enhancers (SSREs)	Tianeptine

Others	Indeloxazine Teniloxazine Tramadol Viqualine

Receptor antagonists and/or reuptake inhibitors

Serotonin antagonists and reuptake inhibitors (SARIs)	Etoperidone Lubazodone Nefazodone Mepiprazole Trazodone

Noradrenergic and specific serotonergic antidepressants (NaSSAs)	Aptazapine Esmirtazapine Mianserin Mirtazapine Setiptiline/Teciptiline

Norepinephrine-dopamine disinhibitors (NDDIs)	Agomelatine

Serotonin modulators and stimulators (SMSs)	Vortioxetine

Others	Tedatioxetine Vilazodone

Heterocyclic antidepressants (bi-, tri-, and tetracyclics)

Bicyclics	Tiazesim Tofenacin

Tricyclics	Amezepine Amineptine Amitriptyline^# Amitriptylinoxide Azepindole Butriptyline Cianopramine Clomipramine^# Cotriptyline Cyanodothiepin Demexiptiline Depramine/Balipramine Desipramine Dibenzepin Dimetacrine Dosulepin/Dothiepin Doxepin Enprazepine Fluotracen Hepzidine Homopipramol Imipramine Imipraminoxide Intriptyline Iprindole Ketipramine Litracen Lofepramine Losindole Mariptiline Melitracen Metapramine Mezepine Naranol Nitroxazepine Nortriptyline Noxiptiline Octriptyline Opipramol Pipofezine Propizepine Protriptyline Quinupramine Tampramine Tianeptine Tienopramine Trimipramine

Tetracyclics	Amoxapine Aptazapine Azipramine Ciclazindol Ciclopramine Esmirtazapine Maprotiline Mazindol Mianserin Mirtazapine Oxaprotiline Setiptiline/Teciptiline

Monoamine oxidase inhibitors (MAOIs)

Nonselective	Irreversible: Benmoxin Carbenzide Cimemoxin Domoxin Echinopsidine Iproclozide Iproniazid Isocarboxazid Mebanazine Metfendrazine Nialamide Octamoxin Phenelzine Pheniprazine Phenoxypropazine Pivalylbenzhydrazine Safrazine Tranylcypromine Reversible: Caroxazone Paraxazone Quercetin

MAO_A-Selective	Irreversible: Clorgiline Reversible: Amiflamine Bazinaprine Befloxatone Berberine Brofaromine Cimoxatone Esuprone Eprobemide Harmala Alkaloids (Harmine Harmaline Tetrahydroharmine Harman Norharman, etc) Methylene Blue Metralindole Minaprine Moclobemide Pirlindole Sercloremine Tetrindole Toloxatone Tyrima

MAO_B-Selective	Irreversible: Ladostigil Mofegiline Pargyline Rasagiline Selegiline Reversible: Lazabemide Milacemide

Azapirones and other 5-HT_1A receptor agonists

Alnespirone Aripiprazole Befiradol Buspirone Eptapirone Flesinoxan Flibanserin Gepirone Ipsapirone Oxaflozane Tandospirone Vilazodone Zalospirone

^#WHO-EM
^‡Withdrawn from market
Clinical trials:
- ^†Phase III
- ^§Never to phase III

M: PSO/PSI

mepr

dsrd (o, p, m, p, a, d, s), sysi/epon, spvo

proc (eval/thrp), drug (N5A/5B/5C/6A/6B/6D)

Anxiolytics (N05B)

GABA_A
PAMs

non-N05B	Alcohols (2M2B, Ethanol (beverage), Ethchlorvynol, Methylpentynol) Chlormezanone Etifoxine Inhalants Kavalactones (Kava) Skullcap Valerenic acid (Valerian)

Benzodiazepine	Adinazolam Alprazolam Bretazenil Bromazepam Camazepam Chlordiazepoxide Clobazam Clonazepam Clorazepate Clotiazepam Cloxazolam Diazepam^# Ethyl Loflazepate Etizolam Fludiazepam Halazepam Imidazenil Ketazolam Lorazepam^# Medazepam Nordazepam Oxazepam Pinazepam Prazepam

Carbamates	Difebarbamate Emylcamate Febarbamate Mebutamate Meprobamate (Carisoprodol, Tybamate) Phenprobamate Procymate

Nonbenzodiazepines	Abecarnil Adipiplon Alpidem CGS-8216 CGS-9896 CGS-13767 CGS-20625 Divaplon ELB-139 Fasiplon GBLD-345 Gedocarnil L-838,417 NS-2664 NS-2710 Ocinaplon Pagoclone Panadiplon Pipequaline RWJ-51204 SB-205,384 SL-651,498 Taniplon TP-003 TP-13 TPA-023 Y-23684 ZK-93423

Pyrazolopyridines	Cartazolate Etazolate ICI-190,622 Tracazolate

α₂δ VDCC Blockers

CRH₁ Antagonists

mGluR₂_/₃ Agonists

mGluR5 NAMs

TSPO agonists

σ₁ agonists

Antidepressants

Others

^#WHO-EM
^‡Withdrawn from market
Clinical trials:
- ^†Phase III
- ^§Never to phase III

M: PSO/PSI

mepr

dsrd (o, p, m, p, a, d, s), sysi/epon, spvo

proc (eval/thrp), drug (N5A/5B/5C/6A/6B/6D)

Neuropeptidergics

Cholecystokinin

CCK_A	Agonists: Cholecystokinin CCK-4 Antagonists: Asperlicin Proglumide Lorglumide Devazepide Dexloxiglumide

CCK_B	Agonists: Cholecystokinin CCK-4 Gastrin Antagonists: Proglumide CI-988

CRH

CRF₁	Agonists: Corticotropin releasing hormone Antagonists: Antalarmin CP-154,526 Pexacerfont

CRF₂	Agonists: Corticotropin releasing hormone

Galanin

GAL₁	Agonists: Galanin Galanin-like peptide Galmic Galnon

GAL₂	Agonists: Galanin Galanin-like peptide Galmic Galnon

GAL₃	Agonists: Galanin Galmic Galnon

Ghrelin

GnRH

MCH

MCH₁	Agonists: Melanin concentrating hormone Antagonists: ATC-0175 GW-803,430 NGD-4715 SNAP-7941 SNAP-94847

MCH₂	Agonists: Melanin concentrating hormone

Melanocortin

MC₁	Agonists: alpha-MSH Afamelanotide BMS-470,539 Bremelanotide Melanotan II Antagonists: Agouti signalling peptide

MC₂	Agonists: ACTH Cosyntropin Tetracosactide

MC₃	Agonists: alpha-MSH Bremelanotide Melanotan II

MC₄	Agonists: alpha-MSH Bremelanotide Melanotan II PF-00446687 THIQ Antagonists: Agouti-related peptide

MC₅	Agonists: alpha-MSH Melanotan II

Neuropeptide S

Agonists: Neuropeptide S
Antagonists: SHA-68

Neuropeptide Y

Y₁	Agonists: Neuropeptide Y Peptide YY Antagonists: BIBP-3226

Y₂	Agonists: Neuropeptide Y Peptide YY Antagonists: BIIE-0246

Y₄	Agonists: Neuropeptide Y Pancreatic polypeptide Peptide YY Antagonists: UR-AK49

Y₅	Agonists: Neuropeptide Y Peptide YY Antagonists: Lu AA-33810

Neurotensin

NTS₁	Agonists: Neurotensin Neuromedin N Antagonists: SR-48692 SR-142,948

NTS₂	Agonists: Neurotensin Antagonists: Levocabastine SR-142,948

Orexin

OX₁	Agonists: Orexin-A Antagonists: Almorexant SB-334,867 SB-408,124 SB-649,868 Suvorexant

OX₂	Agonists: Orexin-A Antagonists: Almorexant SB-649,868 Suvorexant TCS-OX2-29

Oxytocin

Tachykinin

NK₁	Agonists: Substance P Antagonists: Aprepitant Befetupitant Casopitant CI-1021 CP-96,345 CP-99,994 CP-122,721 Dapitant Ezlopitant FK-888 Fosaprepitant GR-203,040 GW-597,599 HSP-117 L-733,060 L-741,671 L-743,310 L-758,298 Lanepitant LY-306,740 Maropitant Netupitant NKP-608 Nolpitantium Orvepitant RP-67,580 SDZ NKT 343 Vestipitant Vofopitant

NK₂	Agonists: Neurokinin A Antagonists: GR-159,897 Ibodutant Saredutant

NK₃	Agonists: Neurokinin B Antagonists: Osanetant Talnetant

Vasopressin

V_1A	Agonists: Desmopressin Felypressin Ornipressin Terlipressin Vasopressin Antagonists: Conivaptan Demeclocycline Relcovaptan

V_1B	Agonists: Felypressin Ornipressin Terlipressin Vasopressin Antagonists: Demeclocycline Nelivaptan

V₂	Agonists: Desmopressin Ornipressin Vasopressin Antagonists: Conivaptan Demeclocycline Lixivaptan Mozavaptan Satavaptan Tolvaptan

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Pexacerfont

See also

References