African Journal of Pharmacy and Pharmacology Vol. 4(6). pp. 289-290, June 2010
Available online http://www.academicjournals.org/ajpp
ISSN 1996-0816 ©2010 Academic Journals
Review
Hypothesis: A promising effect of 5-HT
1A
receptor
agonists in alleviating motor symptoms of Parkinson’s
disease
A. M. Nayebi*
Department of Pharmacology and Toxicology, Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz
51664, Iran. E-mail: nayebia@yahoo.com.
Accepted 13 April, 2010
Parkinson's disease (PD) is a disease caused by degeneration of dopaminergic neurons of substantia
nigra, pars compacta. The fact that serotonergic system is also involved in PD has been raised from
previous studies. Drugs that have effect on 5-HT
1A
receptors of basal ganglia might inhibit and facilitate
serotonin and dopamine release, respectively. Augmentation of 5-HT
1A
agonists (e.g., buspirone) to anti-
parkinsonian and neuroleptic drugs (D2 receptor blockers) may increase efficiency of anti-parkinsonian
drugs and may also prevent motor complications induced by neuroleptic drugs.
Key words: 5-HT
1A
receptor, motor symptom, Parkinson disease.
INTRODUCTION
Parkinson’s disease (PD) is a progressive neuro-
degenerative disease occurring approximately 1% of
population over the age of 50 years. Its most prominent
symptoms are tremor, muscle stiffness and bradykinesia.
Some non-motor symptoms such as cognitive impair-
ment, anxiety and depression usually coexist - comorbid.
The disease is accompanied by preferential loss of dopa-
minergic neurons of the substanitia nigra pars compacta
(SNc) (Scholtissen et al., 2006).
However, other neurotransmitters such as serotonin
are also involved in the neurobiology of PD (Miyawaki et
al., 1997). There are some reports stating that 5-HT
exerts an inhibitory effect on striatal dopamine (DA)
release (De Deurwaerdere et al., 2004). 5-HT
1A
receptors
are widely distributed through-out the basal ganglia
(Vollenweider et al., 1999).
They are located in dorsal raphe neurons with efferents
to the striatum, and are also localized on cortical neurons
sending glutamatergic projections to the basal ganglia
(Knobelman et al., 2000). Recent studies have shown
that 5-HT
1A
receptor stimulation represented antiparkin-
sonian effects in 6-OHDA (6-hydroxydopamine) lesioned
rats (Dupre et al., 2007; Mignon and Wolf, 2007; Nayebi
et al., 2010).
The findings of a clinical study showed that 5-HT
1A
receptor stimulation in levodopa-treated parkinsonian
patients can ameliorate motor fluctuations and dyski-
nesias (Bara-Jimenez et al., 2005). This effect is most
likely caused by the increase in 5-HT
1A
receptor
activation, resulting in an inhibition of serotonin release
(Riad et al., 2000). Stimulation of 5-HT
1A
receptor is asso-
ciated with an increase in dopamine turn-over (Hamon et
al., 1988) and release (Ichikawa and Meltzer, 1999) from
various brain regions, suggesting that 5-HT
1A
agonists
might have potential therapeutic value in the treatment of
PD.
This hypothesis is supported by the finding that 5-HT
1A
agonists can facilitate dopamine release in the striatum
(Benloucif and Galloway, 1991). Therefore, adjuvant
therapy with 5-HT
1A
receptor partial agonists such as
buspirone in addition to being effective in reducing
symptoms of anxiety probably will be able to decrease
movement complications of PD as well as neuroleptic
drugs (D2 receptor blockers).
According to the above information, 5-HT
1A
receptor
agonists may decrease release of serotonin from dorsal
raphe nucleus neurons and subsequently facilitate striatal
dopamine release. We suggest that 5-HT
1A
receptor
agonists may have beneficial effect on treating some
motor complications of PD disease and motor disorders
induced by neuroleptic drugs (e.g. haloperidol). However,
further preclinical and clinical investigations should be
carried out to test their usefulness in diminishing motor
disorders of PD.