T62

Names

[ Name ]:
T62

[Synonym ]:
2-Amino-3-(4-chlorobenzoyl)-5,6,7,8-tetrahydrobenzothiophene
UNII-9Q765ZIF8L
(2-Amino-4,5,6,7-tetrahydrobenzo[b]thiophen-3-yl)(4-chlorophenyl)methanone
T62
(2-amino-4,5,6,7-tetrahydro-1-benzothien-3-yl)(4-chlorophenyl)methanone

Biological Activity

[Description]:

Adenosine A1 receptor activator T62 is an allosteric enhancer of adenosine A1 receptor. Adenosine A1 receptor activator T62 produces antinociception in animal models of acute pain and also reduces hypersensitivity in models of inflammatory and nerve-injury pain[1][2][3].

[Related Catalog]:

Research Areas >> Inflammation/Immunology

Research Areas >> Neurological Disease

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

[Target]

Adenosine A1 receptor[1]

[In Vivo]

Adenosine A1 receptor activator T62 (0.3-3 μg; intrathecal administration; male SpragueDawley rats) treatment produces a dose-dependent antihypersensitivity effect, with no effect on ambulation or activity level[1]. Animal Model: Male SpragueDawley rats (250 g) after paw incision surgery[1] Dosage: 0.3 μg, 0.5 μg, 1 μg, and 3 μg Administration: Intrathecal administration Result: Produced a dose-dependent antihypersensitivity effect, with no effect on ambulation or activity level. The ED40 (95% confidence interval) was 0.77 (0.63-0.91) μg.

[References]

[1]. Obata H, et al. Spinal adenosine receptor activation reduces hypersensitivity after surgery by a different mechanism than after nerve injury. Anesthesiology. 2004 May;100(5):1258-62.

[2]. Li X, et al. Allosteric adenosine receptor modulation reduces hypersensitivity following peripheral inflammation by a central mechanism. J Pharmacol Exp Ther. 2003 Jun;305(3):950-5.

[3]. Soudijn W, et al. Allosteric modulation of G protein-coupled receptors: perspectives and recent developments. Drug Discov Today. 2004 Sep 1;9(17):752-8.

Chemical & Physical Properties

[ Density]:
1.337g/cm3

[ Boiling Point ]:
527ºC at 760 mmHg

[ Molecular Formula ]:
C₁₅H₁₄ClNOS

[ Molecular Weight ]:
291.79600

[ Flash Point ]:
272.5ºC

[ Exact Mass ]:
291.04800

[ PSA ]:
71.33000

[ LogP ]:
4.67470

[ Index of Refraction ]:
1.658

MSDS

Click to get detail MSDS

Safety Information

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

[ RIDADR ]:
NONH for all modes of transport

[ WGK Germany ]:
3

[ HS Code ]:
2934999090

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Customs

[ HS Code ]: 2934999090

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Articles

Allosteric adenosine receptor modulation reduces hypersensitivity following peripheral inflammation by a central mechanism.

J. Pharmacol. Exp. Ther. 305 , 950-955, (2003)

Activation of adenosine A1 receptors by endogenous adenosine or synthetic agonists produces antinociception in animal models of acute pain and also reduces hypersensitivity in models of inflammatory a...

Repeated dosing with oral allosteric modulator of adenosine A1 receptor produces tolerance in rats with neuropathic pain.

Anesthesiology 100(4) , 956-61, (2004)

The positive allosteric adenosine receptor modulator, T62 (2-amino-3-(4-chlorobenzoyl)-5,6,7,8-tetrahydrobenzothiophene), has been shown to reduce mechanical allodynia in a rat model of neuropathic pa...

Allosteric modulation of G protein-coupled receptors: perspectives and recent developments.

Drug Discov. Today 9 , 752-758, (2004)

Allosteric modulation of G protein-coupled receptors has recently been recognized as an alternative approach to gain selectivity in drug action. In this overview, allosteric modulators that enhance or...

Related Compounds

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