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Table 1 Common agonists and antagonists of 5-HT7R used in preclinical studies

From: Central nervous system effects of 5-HT7 receptors: a potential target for neurodegenerative diseases

Name

Action mechanism

Administration route (dose)

References

AS-19

Selective full agonist

s.c (5 mg/kg), i.t. (5 µL at 100 µM), i.p. (10 mg/kg)

McDaid et al. (2020), Fields et al. (2015), Albayrak et al. (2013)

LP-12

Selective full agonist

i.t. (10µL at 0.02–0.2 nM), cultures (300 nM)

Godínez-Chaparro et al. (2012), Samarajeewa et al. (2014)

LP-44

Selective full agonist

i.p. (1,5 and 10 mg/kg)

Demirkaya et al. (2016)

LP-211

Selective full agonist

i.p. (1,5 and 10 mg/kg), i.p. (0.25 mg/kg), i.p. (0.003–0.3 mg/kg),i.c.v. (0.2 µL at 2–6 mM)

Demirkaya et al. (2016), Liu et al. (2021), Norouzi-Javidan et al. (2016), (Monti et al. 2014)

Methiothepin maleate

Non-specific 5-HT1/6/7R agonist

Culture (10 µM)

Soga et al. (2007)

8-OH-DPAT

Non-specific 5-HT1A/7R agonist

i.p. (02–0.4 mg/kg and 1.0 mg/kg)

Cassaday and Thur (2019), Odland et al. (2019)

SB-269970

Competitive selective antagonist, quasi-full inverse agonist

i.p. (10 mg/kg)

Perez-García and Meneses (2005), Liu et al. (2021)

SB-258741

Competitive selective antagonist, partial inverse agonist

s.c. (2.3 mg/kg and 3.5 mg/kg)

Pouzet (2002)

SB-258719

Competitive selective antagonist

i.p. (5 mg/kg)

Brenchat et al. (2011)

HBK-15

Competitive non-selective

5-HT1A/3/7R antagonist

i.p. (1.25 mg/kg) i.v. (1.25 mg/kg)

Pytka et al. (2018)

Lurasidone

Competitive non-selective 5-HT2A/7R antagonist

Microdialsis (3 mg/kg/d)

Okada et al. (2021)