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5-HT4 antagonist 1

Names

[ CAS No. ]:
261766-73-8

[ Name ]:
5-HT4 antagonist 1

Biological Activity

[Description]:

5-HT4 antagonist 1 is a 5-HT4 receptor antagonist with a pKi of 9.6.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor
Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor
Research Areas >> Neurological Disease

[Target]

pKI: 9.6 (5-HT4 receptor)[1]


[In Vitro]

5-HT4 antagonist 1 (compound 6b) is a 5-HT4 receptor antagonist with a pKi of 9.6.

[In Vivo]

5-HT4 antagonist 1 (compound 6b) demonstrates good exposure and prolongs t1/2 in other species, including the mouse (t1/2 7 h), rat (t1/2 12 h) and mini-pig (t1/2 21 h). In Phase I clinical trial, it is found that 5-HT4 antagonist 1 has good oral bioavailability with a steady state plasma t1/2 of >100 h[1].

[References]

[1]. Clark RD, et al. Identification of a 5-HT4 receptor antagonist clinical candidate through side-chain modification. Bioorg Med Chem Lett. 2005 Mar 15;15(6):1697-700.


[Related Small Molecules]

Harmine | Pimavanserin | Serotonin hydrochloride | Sodium Ferulate | Thioridazine hydrochloride | Brexpiprazole | Risperidone | TG6-10-1 | Cariprazine | Quetiapine | SERTINDOLE | Alprenolol hydrochloride | B-HT 920 | Ketanserin | Palonosetron hydrochloride

Chemical & Physical Properties

[ Molecular Formula ]:
C23H36N4O5S

[ Molecular Weight ]:
480.62

[ Storage condition ]:
2-8℃

Related Compounds