587870-77-7
587870-77-7 structure
- Name: ABT 724 trihydrochloride
- Chemical Name: 2-{[4-(2-Pyridinyl)-1-piperazinyl]methyl}-1H-benzimidazole trihydrochloride
- CAS Number: 587870-77-7
- Molecular Formula: C17H22Cl3N5
- Molecular Weight: 402.749
- Catalog: Signaling Pathways GPCR/G Protein Dopamine Receptor
- Create Date: 2018-07-03 01:50:19
- Modify Date: 2024-01-12 20:31:24
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ABT-724 trihydrochloride is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 trihydrochloride is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM), and has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 trihydrochloride could be useful for the treatment of erectile dysfunction and has favorable side-effect profile[1].
| Name | 2-{[4-(2-Pyridinyl)-1-piperazinyl]methyl}-1H-benzimidazole trihydrochloride |
|---|---|
| Synonyms |
MFCD08703101
1H-Benzimidazole, 2-[[4-(2-pyridinyl)-1-piperazinyl]methyl]-, hydrochloride (1:3) 2-{[4-(2-Pyridinyl)-1-piperazinyl]methyl}-1H-benzimidazole trihydrochloride 2-{[4-(Pyridin-2-yl)piperazin-1-yl]methyl}-1H-benzimidazole trihydrochloride ABT-724 trihydrochloride |
| Description | ABT-724 trihydrochloride is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 trihydrochloride is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM), and has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 trihydrochloride could be useful for the treatment of erectile dysfunction and has favorable side-effect profile[1]. |
|---|---|
| Related Catalog | |
| Target |
EC50: 12.4 nM (Human dopamine D4 receptor), 14.3 nM (Rat dopamine D4 receptor) and 23.2 nM (Ferret dopamine D4 receptor)[1] |
| In Vitro | ABT-724 exhibits a selective biochemical profile, as indicates by a lack of binding affinity for >70 neurotransmitter/uptake/ion channels including D2, D3, or D5 receptors up to a 10 μM concentration. A weak affinity to 5-HT1A receptors (Ki = 2780 nM) is observed. ABT-724 does not inhibit the PDE activity of PDE1, PDE5, or PDE6 at 10 μM concentrations[1]. |
| In Vivo | ABT-724 (8.8 μg/kg; subcutaneous injection; daily; for 5 days; male adult Wistar rats) treatment dose-dependently facilitates penile erection when given s.c. to conscious rats[1]. Animal Model: Male adult Wistar rats (~300 g)[1] Dosage: 8.8 μg/kg Administration: Subcutaneous injection; daily; for 5 days Result: Dose-dependently facilitated penile erection. |
| References |
| Molecular Formula | C17H22Cl3N5 |
|---|---|
| Molecular Weight | 402.749 |
| Exact Mass | 401.094086 |
| Symbol |
GHS07 |
|---|---|
| Signal Word | Warning |
| Hazard Statements | H315-H319-H335 |
| Precautionary Statements | P261-P305 + P351 + P338 |
| RIDADR | NONH for all modes of transport |