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ABT 102

ABT 102

  • CAT Number: I000742
  • CAS Number: 808756-71-0
  • Molecular Formula: C21H24N4O
  • Molecular Weight: 348.45
  • Purity: ≥95%
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ABT-102(CAT: I000742) is a selective and potent inhibitor of the histamine H3 receptor. The histamine H3 receptor is primarily found in the central nervous system and is involved in regulating neurotransmitter release, including the modulation of histamine, dopamine, and other neurotransmitters. By inhibiting the H3 receptor, ABT-102 may affect neurotransmission, leading to potential therapeutic effects in conditions such as cognitive disorders, sleep disorders, and psychiatric conditions.

Catalog Number I000742
CAS Number 808756-71-0
Synonyms

ABT 102; ABT-102; ABT102; CHEMBL398338;;Urea, N-((1R)-5-(1,1-dimethylethyl)-2,3-dihydro-1H-inden-1-yl)-N/’-1H-indazol-4-yl-

Molecular Formula

C21H24N4O

Purity 95%
Target TRPV1 Antagonist
Solubility Soluble in DMSO, not in water
Storage 0 - 4°Cfor short term (days to weeks), or -20 °C for long term (months).
IUPAC Name 1-[(1R)-5-tert-butyl-2,3-dihydro-1H-inden-1-yl]-3-(1H-indazol-4-yl)urea
InChI InChI=1S/C21H24N4O/c1-21(2,3)14-8-9-15-13(11-14)7-10-18(15)24-20(26)23-17-5-4-6-19-16(17)12-22-25-19/h4-6,8-9,11-12,18H,7,10H2,1-3H3,(H,22,25)(H2,23,24,26)/t18-/m1/s1
InChIKey TYOYXJNGINZFET-GOSISDBHSA-N
SMILES CC(C)(C)C1=CC2=C(C=C1)C(CC2)NC(=O)NC3=CC=CC4=C3C=NN4
Reference

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1:Solid state drug-polymer miscibility studies using the model drug ABT-102. Jog R, Gokhale R, Burgess DJ.Int J Pharm. 2016 Jul 25;509(1-2):285-95. doi: 10.1016/j.ijpharm.2016.05.068. Epub 2016 Jun 3. PMID: 27265312 <br />
2:Formulation design and evaluation of amorphous ABT-102 nanoparticles. Jog R, Kumar S, Shen J, Jugade N, Tan DC, Gokhale R, Burgess DJ.Int J Pharm. 2016 Feb 10;498(1-2):153-69. doi: 10.1016/j.ijpharm.2015.12.033. Epub 2015 Dec 15. PMID: 26705150 <br />
3:The amorphous solid dispersion of the poorly soluble ABT-102 forms nano/microparticulate structures in aqueous medium: impact on solubility. Frank KJ, Westedt U, Rosenblatt KM, H&#246;lig P, Rosenberg J, M&#228;gerlein M, Fricker G, Brandl M.Int J Nanomedicine. 2012;7:5757-68. doi: 10.2147/IJN.S36571. Epub 2012 Nov 12. PMID: 23166440 Free PMC Article<br />
4:Effects of the TRPV1 antagonist ABT-102 on body temperature in healthy volunteers: pharmacokinetic/ pharmacodynamic analysis of three phase 1 trials. Othman AA, Nothaft W, Awni WM, Dutta S.Br J Clin Pharmacol. 2013 Apr;75(4):1029-40. doi: 10.1111/j.1365-2125.2012.04405.x. PMID: 22966986 Free PMC Article<br />
5:Amorphous solid dispersion enhances permeation of poorly soluble ABT-102: true supersaturation vs. apparent solubility enhancement. Frank KJ, Rosenblatt KM, Westedt U, H&#246;lig P, Rosenberg J, M&#228;gerlein M, Fricker G, Brandl M.Int J Pharm. 2012 Nov 1;437(1-2):288-93. doi: 10.1016/j.ijpharm.2012.08.014. Epub 2012 Aug 20. PMID: 22951865 <br />
6:A Phase 1 Study to Evaluate the Bioavailability and Food Effect of 2 Solid-Dispersion Formulations of the TRPV1 Antagonist ABT-102, Relative to the Oral Solution Formulation, in Healthy Human Volunteers. Othman AA, Cheskin H, Locke C, Nothaft W, Dutta S.Clin Pharmacol Drug Dev. 2012 Jan;1(1):24-31. doi: 10.1177/2160763X11430860. PMID: 27206143 <br />
7:Pharmacokinetics of the TRPV1 antagonist ABT-102 in healthy human volunteers: population analysis of data from 3 phase 1 trials. Othman AA, Nothaft W, Awni WM, Dutta S.J Clin Pharmacol. 2012 Jul;52(7):1028-41. doi: 10.1177/0091270011407497. Epub 2011 May 12. PMID: 21566201 <br />
8:Oral and cutaneous thermosensory profile of selective TRPV1 inhibition by ABT-102 in a randomized healthy volunteer trial. Rowbotham MC, Nothaft W, Duan WR, Wang Y, Faltynek C, McGaraughty S, Chu KL, Svensson P.Pain. 2011 May;152(5):1192-200. doi: 10.1016/j.pain.2011.01.051. Epub 2011 Mar 4. PMID: 21377273 <br />
9:Repeated dosing of ABT-102, a potent and selective TRPV1 antagonist, enhances TRPV1-mediated analgesic activity in rodents, but attenuates antagonist-induced hyperthermia. Honore P, Chandran P, Hernandez G, Gauvin DM, Mikusa JP, Zhong C, Joshi SK, Ghilardi JR, Sevcik MA, Fryer RM, Segreti JA, Banfor PN, Marsh K, Neelands T, Bayburt E, Daanen JF, Gomtsyan A, Lee CH, Kort ME, Reilly RM, Surowy CS, Kym PR, Mantyh PW, Sullivan JP, Jarvis MF, Faltynek CR.Pain. 2009 Mar;142(1-2):27-35. doi: 10.1016/j.pain.2008.11.004. Epub 2009 Jan 9. PMID: 19135797 <br />
10:(R)-(5-tert-butyl-2,3-dihydro-1H-inden-1-yl)-3-(1H-indazol-4-yl)-urea (ABT-102) blocks polymodal activation of transient receptor potential vanilloid 1 receptors in vitro and heat-evoked firing of spinal dorsal horn neurons in vivo. Surowy CS, Neelands TR, Bianchi BR, McGaraughty S, El Kouhen R, Han P, Chu KL, McDonald HA, Vos M, Niforatos W, Bayburt EK, Gomtsyan A, Lee CH, Honore P, Sullivan JP, Jarvis MF, Faltynek CR.J Pharmacol Exp Ther. 2008 Sep;326(3):879-88. doi: 10.1124/jpet.108.138511. Epub 2008 May 30. PMID: 18515644 Free Article

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