For research use only. Not for therapeutic Use.
Alverine citrate is a 5-HT1A receptor antagonist, with an IC50 of 101 nM.
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].
| Catalog Number | I004072 |
| CAS Number | 5560-59-8 |
| Synonyms | N-ethyl-3-phenyl-N-(3-phenylpropyl)propan-1-amine;2-hydroxypropane-1,2,3-tricarboxylic acid |
| Molecular Formula | C26H35NO7 |
| Purity | ≥95% |
| InChI | InChI=1S/C20H27N.C6H8O7/c1-2-21(17-9-15-19-11-5-3-6-12-19)18-10-16-20-13-7-4-8-14-20;7-3(8)1-6(13,5(11)12)2-4(9)10/h3-8,11-14H,2,9-10,15-18H2,1H3;13H,1-2H2,(H,7,8)(H,9,10)(H,11,12) |
| InChIKey | RYHCACJBKCOBTJ-UHFFFAOYSA-N |
| SMILES | CCN(CCCC1=CC=CC=C1)CCCC2=CC=CC=C2.C(C(=O)O)C(CC(=O)O)(C(=O)O)O |
| Reference | [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. |
