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Chemical Structure| 220953-69-5 Chemical Structure| 220953-69-5

Structure of Antalarmin HCl
CAS No.: 220953-69-5

Chemical Structure| 220953-69-5

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Antalarmin (hydrochloride) is a non-peptide antagonist of corticotropin-releasing hormone receptor 1 (CRHR1) with a Ki of 1 nM.

Synonyms: Antalarmin (hydrochloride); Antalarmin hydrochloride

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Product Details of Antalarmin HCl

CAS No. :220953-69-5
Formula : C24H35ClN4
M.W : 415.01
SMILES Code : CC1=C(C)C2=C(N(CCCC)CC)N=C(C)N=C2N1C3=C(C)C=C(C)C=C3C.[H]Cl
Synonyms :
Antalarmin (hydrochloride); Antalarmin hydrochloride
MDL No. :MFCD05664721

Safety of Antalarmin HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of Antalarmin HCl

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
COS-M6 cells 10 µM 15 min Measure intracellular cAMP levels, Antalarmin blocks the constitutive activation of CRF(1–16)-R1DN chimera in a dose-dependent manner Proc Natl Acad Sci U S A. 2000 Aug 29;97(18):10277-81
dlBnST neurons 40 or 4μM 45 min To test the effect of antalarmin on the frequency of GABA A receptor-mediated spontaneous inhibitory postsynaptic currents (sIPSCs). Results showed that antalarmin significantly reduced the frequency of sIPSCs in the AAS-treated group, reversing the AAS-induced enhancement of GABAergic inhibition. Neuropsychopharmacology. 2012 May;37(6):1483-99

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Balb/c mice Orthotopic injection of 4T1 cells in the mammary fat pad to induce breast tumors Intraperitoneal injection 20 mg/kg Daily for 6 weeks To assess the impact of peripheral CRF inhibition on stress-induced tumor growth, results showed that Antalarmin suppressed stress-induced tumor growth and neoangiogenesis. Mol Cancer. 2010 Sep 27;9:261
Sprague-Dawley rats Stress and anxiety-related behavior model Intraperitoneal injection 20 mg/kg Single administration To evaluate whether antalarmin could mitigate the attention deficits induced by PACAP. Results showed that antalarmin attenuated, but did not completely reverse, the effects of PACAP. Biol Psychiatry. 2016 Dec 15;80(12):955-964
Rats Ethanol-dependent model Intraperitoneal injection 10 or 20 mg/kg Single administration, 1 hour (80 minutes) prior to testing Antalarmin significantly reduced ethanol self-administration in ethanol-dependent rats during acute withdrawal but had no effect in nondependent rats. Biol Psychiatry. 2007 Jan 1;61(1):78-86
Adult male rhesus macaques Social stress model (intruder paradigm) Oral 20 mg/kg Single dose, behavioral assessment 150 minutes post-administration To evaluate the effects of Antalarmin on behavioral, neuroendocrine, and autonomic responses to stress in rhesus macaques. Results showed that Antalarmin significantly reduced anxiety and fear-related behaviors, increased exploratory and sexual behaviors, and significantly attenuated the increases in cerebrospinal fluid CRH as well as the pituitary-adrenal, sympathetic, and adrenal medullary responses to stress. Proc Natl Acad Sci U S A. 2000 May 23;97(11):6079-84
Mice Environmental switch model Intraperitoneal injection 10 mg/kg Twice daily for 7 days Blockade of CRF1R completely eliminated the enhancement of cocaine rewarding effects induced by environmental switch Neuropsychopharmacology. 2012 Jun;37(7):1579-87
Rats Swim stress model Intraperitoneal injection 32 mg/kg Single administration, swim test lasted for 2 hours To evaluate the effect of Antalarmin on cardiac vagal activity during swim stress. Results showed that Antalarmin significantly prolonged PR interval, induced severe bradycardia, and increased the percentage of sinking rats. These effects were blocked by methylatropine nitrate. Neuropsychopharmacology. 2006 Dec;31(12):2580-90
Wistar rats Fear memory retrieval model Intra-MRN injection 250 ng Single injection, 10 minutes before To evaluate the role of CRF1 receptor in fear memory retrieval, results showed no significant effect of Antalarmin on freezing behavior Neuropsychopharmacology. 2010 May;35(6):1271-8
Female C57BL/6J mice Chronic AAS exposure-induced anxiety-like behavior model Intracerebroventricular (i.c.v.) infusion 10 mg/kg Single injection, 5 minutes before testing To evaluate the blocking effect of antalarmin on AAS-induced anxiety-like behaviors. Results showed that antalarmin significantly blocked the AAS-induced increase in ASR amplitudes, indicating that CRF-R1 signaling plays a key role in AAS-induced anxiety. Neuropsychopharmacology. 2012 May;37(6):1483-99

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.41mL

0.48mL

0.24mL

12.05mL

2.41mL

1.20mL

24.10mL

4.82mL

2.41mL

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