Terodiline

Names

[ Name ]:
Terodiline

[Synonym ]:
RS-terodiline
Terodilina
Bicor
Terodiline
2-tert-Butylamino-4,4-diphenylbutan
Terodilinum
RARECHEM AN KC 0196

Biological Activity

[Description]:

Terodiline is an M1-selective muscarinic receptor (mAChR) antagonist with Kbs of 15, 160, 280, and 198 nM in rabbit vas deferens (M1), atria (M2), bladder (M3) and ileal muscle (M3), respectively. Terodiline also is a Ca2+ blocker. Terodiline acts as a treatment for urinary frequency and urge incontinence[1].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> Calcium Channel

Signaling Pathways >> Neuronal Signaling >> mAChR

Signaling Pathways >> GPCR/G Protein >> mAChR

Research Areas >> Neurological Disease

[Target]

mAChR[1] Ca2+ channel[1]

[In Vivo]

Terodiline (80 mg/kg; S.C.) is equipotent in inhibiting intravesical bladder pressure and carbachol-induced salivary secretion (ID50= 24 and 35 mg/kg, respectively), and in increasing pupil diameter (ED50=59 mg/kg)[1]. Animal Model: Fmale or male Hartley guinea pigs (200-600 g)[1] Dosage: 80 mg/kg Administration: Administered S.C. Result: Yielded an ID50 of 24±6 mg/kg. Higher doses were Iethal.

[References]

[1]. Noronha-Blob L, et al. (+/-)-Terodiline: an M1-selective muscarinic receptor antagonist. In vivo effects at muscarinic receptors mediating urinary bladder contraction, mydriasis and salivary secretion. Eur J Pharmacol. 1991 Aug 29;201(2-3):135-42.

Chemical & Physical Properties

[ Density]:
0.956g/cm3

[ Boiling Point ]:
390.9ºC at 760mmHg

[ Molecular Formula ]:
C₂₀H₂₇N

[ Molecular Weight ]:
281.44

[ Flash Point ]:
168.9ºC

[ Exact Mass ]:
225.15200

[ PSA ]:
26.02000

[ LogP ]:
4.25610

[ Vapour Pressure ]:
2.57E-06mmHg at 25°C

[ Index of Refraction ]:
1.534

Safety Information

[ HS Code ]:
2921499090

Customs

[ HS Code ]: 2921499090

[ Summary ]:
2921499090 other aromatic monoamines and their derivatives; salts thereof VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:30.0%