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5560-59-8

5560-59-8 structure
5560-59-8 structure

Name alverine citrate
Synonyms N-ethyl-3-phenyl-N-(3-phenylpropyl)propan-1-amine,2-hydroxypropane-1,2,3-tricarboxylic acid
MFCD00035086
EINECS 226-929-3
Alverine Citrate
Alverine (citrate)
Description Alverine citrate is a 5-HT1A receptor antagonist, with an IC50 of 101 nM.
Related Catalog
Target

5-HT1A Receptor:101 nM (IC50)

In Vitro Alverine is a drug used for functional gastrointestinal disorders. Alverine acts directly on the muscle in the gut, causing it to relax. Alverine Citrate (20 mg/kg) suppresses the effect of 5-HTP, but not that of 8-OH-DPAT. However, when injected intracerebroventricularly (75 μg/rat) alverine citrate reduces 8-OH-DPAT-induced enhancement of rectal distension-induced abdominal contractions. In-vitro binding studies reveal that Alverine citrate has a high affinity for 5-HT1A receptors and a weak affinity for 5-HT3 and 5-HT4 subtypes[1]. Alverine may increase Ca influx during action potentials due to inhibition of the inactivation of L-type Ca channels, but may also suppress evoked activity by inhibiting the sensitivity of contractile proteins to Ca2+[2].
References

[1]. Coelho, A.M., et al., Rectal antinociceptive properties of alverine citrate are linked to antagonism at the 5-HT1A receptor subtype. J Pharm Pharmacol, 2001. 53(10): p. 1419-26.

[2]. Hayase, M., et al., Evolving mechanisms of action of alverine citrate on phasic smooth muscles. Br J Pharmacol, 2007. 152(8): p. 1228-38.

Boiling Point 358.8ºC at 760mmHg
Molecular Formula C26H35NO7
Molecular Weight 473.55900
Flash Point 174.4ºC
Exact Mass 473.24100
PSA 135.37000
LogP 3.32540
Storage condition -20°C
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 2921499090
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%