AGI-001

Names

[ Name ]:
AGI-001

[Synonym ]:
Tocris-1060
(2S)-1-(1H-indol-4-yloxy)-3-(propan-2-ylamino)propan-2-ol
DL-AP4 Sodium salt

Biological Activity

[Description]:

l-Pindolol ((-)-pindolol) is a reversible, competitive and orally active 5-HT1A/1B antagonist. l-Pindolol is a partial β-adrenoceptor agonist. l-Pindolol can be used for the research of neurological disease[1][2][3].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[In Vitro]

l-Pindolol (500 nM 和 1 μM) 拮抗 5-羧胺色胺 (5-CT；10 nM) 和 5-羟色胺 (5-HT；15 μM) 通过检测 5-CT 和 5-HT 对 CA1 锥体细胞的膜超极化[1]。 l-Pindolol (1 nM-100 μM) 抑制 100 nM 5-CT 诱导的 CA1 锥体细胞超极化，IC50 值为 92 nM[1]。 l-Pindolol (1 nM-100 μM) 抑制 300 nM 5-CT 引起的 CA3 神经元超极化，IC50 值为 522 nM[1]。

[In Vivo]

l-Pindolol (15 mg/kg；腹腔注射，[3H]-WAY 100635 注射前预处理) 减少了 [3H]-WAY 100635 在含有 5-HT1A 受体的脑区的积累。 Animal Model: Male Sprague Dawley rats[1] Dosage: 15 mg/kg Administration: Intraperitoneal injection; 15 mg/kg, 20 min acute treatment or 24 h, 16 h and 20 min short-term treatment before [3H]-WAY 100635 injection Result: Reduced [3H]-WAY 100635 accumulation in 5-HT1A receptor-containing brain areas, but showed no effect on the dorsal raphe nucleus (DRN), and the CA1 and CA3 hippocampal areas.

Chemical & Physical Properties

[ Density]:
1.152g/cm3

[ Boiling Point ]:
457.1ºC at 760mmHg

[ Molecular Formula ]:
C₁₄H₂₀N₂O₂

[ Molecular Weight ]:
248.32100

[ Exact Mass ]:
248.15200

[ PSA ]:
57.28000

[ LogP ]:
2.29650

[ Vapour Pressure ]:
3.77E-09mmHg at 25°C

[ Index of Refraction ]:
1.596

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

[ HS Code ]:
2933990090

Customs

[ HS Code ]: 2933990090

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Articles

Chemical genetics reveals a complex functional ground state of neural stem cells.

Nat. Chem. Biol. 3(5) , 268-273, (2007)

The identification of self-renewing and multipotent neural stem cells (NSCs) in the mammalian brain holds promise for the treatment of neurological diseases and has yielded new insight into brain canc...

Loss of [125I]-pindolol binding to beta-adrenoceptors on rat nodose ganglion after chronic isoprenaline treatment.

J. Auton. Nerv. Syst. 60 , 12-16, (1996)

The nodose ganglion contains the cell bodies of afferent nerves which convey predominantly sensory information from the viscera to the central nervous system (CNS). Autoradiographic studies show bindi...

Pindolol suppresses serotonergic neuronal activity and does not block the inhibition of serotonergic neurons produced by 8-hydroxy-2-(di-n-propylamino)tetralin in awake cats.

J. Pharmacol. Exp. Ther. 291 , 229, (1999)

Clinical studies have shown that pindolol can enhance the effects of antidepressant drugs, presumably by acting as an antagonist at somatodendritic 5-hydroxytryptamine (5-HT)(1A) autoreceptors, which ...