180084-26-8
180084-26-8 structure
- Name: SB 224289 hydrochloride
- Chemical Name: [4-[2-methyl-4-(5-methyl-1,2,4-oxadiazol-3-yl)phenyl]phenyl]-(1'-methylspiro[6,7-dihydro-2H-furo[2,3-f]indole-3,4'-piperidine]-5-yl)methanone,hydrochloride
- CAS Number: 180084-26-8
- Molecular Formula: C32H33ClN4O3
- Molecular Weight: 557.082
- Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
- Create Date: 2017-11-14 03:35:07
- Modify Date: 2024-01-22 09:54:01
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SB-224289 hydrochloride is a selective 5-HT1B receptor antagonist, with anxiolytic effect.
| Name | [4-[2-methyl-4-(5-methyl-1,2,4-oxadiazol-3-yl)phenyl]phenyl]-(1'-methylspiro[6,7-dihydro-2H-furo[2,3-f]indole-3,4'-piperidine]-5-yl)methanone,hydrochloride |
|---|---|
| Synonyms |
(1'-Methyl-6,7-dihydro-5H-spiro[furo[2,3-f]indole-3,4'-piperidin]-5-yl)[2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methanone hydrochloride (1:1)
1'-Methyl-5-[[2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydrospiro[furo[2,3-f]indole-3,4'-piperidine] hydrochloride Methanone, (6,7-dihydro-1'-methylspiro[2H-furo[2,3-f]indole-3(5H),4'-piperidin]-5-yl)[2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)[1,1'-biphenyl]-4-yl]-, hydrochloride (1:1) (1'-Methyl-6,7-dihydro-5H-spiro[furo[2,3-f]indole-3,4'-piperidin]-5-yl)[2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)-4-biphenylyl]methanone hydrochloride (1:1) SB 224289 hydrochloride SB-224289 hydrochloride |
| Description | SB-224289 hydrochloride is a selective 5-HT1B receptor antagonist, with anxiolytic effect. |
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| Related Catalog | |
| Target |
5-HT1B receptor[2] |
| In Vitro | SB-224289 has specific toxin-blocking ability and does not inhibit Cho1p. SB-224289 (100 μM-25 μM) shows consistent efficacy at producing Pap-A resistance. SB-224289 does not directly inhibit the PS synthase enzyme in this in vitro assay. Moreover, SB-224289 specifically blocks the activity of papuamides and not other membrane disruptors. SB-224289 is unable to protect wild-type cells against KF, but it is able to provide protection against TPap-A[1]. SB-224289 has a pKi of 8 at human cloned 5-HT1B receptors and displays more than 80 fold selectivity over the closely related 5-HT1D receptor and a range of other receptors. SB-224289 is a potent antagonist with pEC50 of 7.9±0.1. SB-224289 evokes a parallel rightward shift in the 5-HT concentration response curve with pA2 of 8.4±0.2. SB-224289 (100 nM and 1 μM) also significantly increases [3H]-5HT release in electrically stimulated guinea-pig brain cortex slices[3]. |
| In Vivo | SB-224289 (SB 224289) alone or in combination with cocaine, increases anxiety-like behavior. SB 224289 significantly reduces the amount of locomotor activity in the cocaine-treated rats. SB 224289-treated animals spend a significantly longer time in the corners than those treated with vehicle[2]. SB 224289 is a potent antagonist with an ED50 of 3.6 mg/kg, p.o in SK&F-99101-induced hypothermia in the guinea-pig. SB 224289 (4 mg/kg, p.o) reverses sumatriptan-induced inhibition of 5-HT release showing that it is also a potent terminal 5-HT autoreceptor antagonist in vivo. SB 224289 (2-16 mg/kg, p.o) does not increase 5-HT levels in the fuinea-pig frontal cortex. However, SB 224289 (4 mg/kg, p.o) causes a significantly increase in levels of 5-HT in the fuinea-pig dentate gyrus[3]. |
| Animal Admin | Ninety minutes before each animal is tested, it receives an ip injection of either 5 mg/kg SB 224289 in a vehicle of 10% Trappsol in sterile water or vehicle alone (total volume 1 mL/kg). This dosage of this drug is effective as a pharmacological agent. The rat is put back in its home cage until just before it is to be tested. |
| References |
| Boiling Point | 724.8ºC at 760 mmHg |
|---|---|
| Molecular Formula | C32H33ClN4O3 |
| Molecular Weight | 557.082 |
| Flash Point | 392.2ºC |
| Exact Mass | 556.224121 |
| PSA | 71.70000 |
| LogP | 6.38400 |
| Vapour Pressure | 7.29E-21mmHg at 25°C |
| Storage condition | 2-8℃ |