Structure of Antalarmin HCl
CAS No.: 220953-69-5
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
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
4.5
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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 |
GHS Pictogram: |
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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 |
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 |
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 |
Tags: Antalarmin | CRFR | Corticotropin-releasing Factor Receptor | CRHR | inhibitor | 220953-69-5 |
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H420 | Harms public health and the environment by destroying ozone in the upper atmosphere |
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