80
5
References
Alagha K, Palot A, Sofalvi T, Pahus L, Gouitaa M, Tummino C, Martinez S, Charpin D, Bourdin A, Chanez P
(2014) Long-acting muscarinic receptor antagonists for the treatment of chronic airway diseases. Ther
Adv Chronic Dis 5:85–98
Barnes PJ (2013) Theophylline. Am J Respir Crit Care Med 188:901–906
Beaulieu JM, Gainetdinov RR (2011) The physiology, signaling, and pharmacology of dopamine receptors.
Pharmacol Rev 63:182–217
Bergamaschi MM, Queiroz RH, Zuardi AW, Crippa JA (2011) Safety and side effects of cannabidiol, a
Cannabis sativa constituent. Curr Drug Saf 6:237–249
Borea PA, Varani K, Vincenzi F, Baraldi PG, Tabrizi MA, Merighi S, Gessi S (2015) The A3 adenosine receptor:
history and perspectives. Pharmacol Rev 67:74–102
Boyd KN, Mailman RB (2012) Dopamine receptor signaling and current and future antipsychotic drugs.
Handb Exp Pharmacol 212:53–86
Brown SP, Safo PK, Regehr WG (2004) Endocannabinoids inhibit transmission at granule cell to Purkinje
cell synapses by modulating three types of presynaptic calcium channels. J Neurosci 24:5623–5631
Catterall WA (2015) Regulation of cardiac calcium channels in the fight-or-flight response. Curr Mol
Pharmacol 8:12–21
extracellular ligand for adenosine receptors, it signals in an energy-dependent
way to induce physiological and psychological responses, such as modulation of
motor activity and sleep.
5 Cannabis (THC) from the plant Cannabis sativa partially agonizes cannabinoid
receptors. Cannabinoid receptors are activated by endogenous cannabinoids
including arachidonoylglycerol and anandamide, both derivatives of arachidonic
acid. They are released from the postsynapse after neurotransmission at both,
activating (glutamate) or inhibiting (GABA) synapses. Cannabinoid receptors at
the presynapse are activated in response and block secretion of the neurotransmitter. This system comprises a paradigm for retrograde neuronal signalling.
5 Cocaine and the synthetic drugs amphetamine and methamphetamine inhibit
the dopamine transporter DAT. DAT is a solute carrier transporter and a Na + /
dopamine symporter. It regulates the availability of dopamine, serotonin and
noradrenalin for synaptic signalling on receptors by transporting it from the
synaptic cleft back into the cell. Its inhibition therefore induces a dopamine
“overflow” and this may cause euphoria and increased activity and performance.
Side effects relate to disturbed uptake of noradrenalin and include increases in
breathing and heart frequency.
5 Hallucinogens include psilocybin, mescaline and the synthetic drug LSD. They
act preferably on 5HT2 A receptors which are GPCRs. Their activation leads to a
robust increase in the activity of pyramidal neurons, which receive input from
brain areas processing sensory information. This induces a sensory and cognitive
overload.
5 Morphine and other opioids bind to opioid receptors. Opioid receptors are activated
by endogenous peptides including enkephalins. They are involved in modulating
pain perception. Morphine is the agonist for the μ-opioid receptors. It has strong
analgesic effects. Acting on opioid receptors in certain brain regions, it also causes
euphoria and feelings of pleasure and reward. On the downside it induces tolerance, addiction and extremely strong withdrawal symptoms after extended usage.
Chapter 5 · GPCRs as Targets for Plant-Derived Drugs
5
References
Alagha K, Palot A, Sofalvi T, Pahus L, Gouitaa M, Tummino C, Martinez S, Charpin D, Bourdin A, Chanez P
(2014) Long-acting muscarinic receptor antagonists for the treatment of chronic airway diseases. Ther
Adv Chronic Dis 5:85–98
Barnes PJ (2013) Theophylline. Am J Respir Crit Care Med 188:901–906
Beaulieu JM, Gainetdinov RR (2011) The physiology, signaling, and pharmacology of dopamine receptors.
Pharmacol Rev 63:182–217
Bergamaschi MM, Queiroz RH, Zuardi AW, Crippa JA (2011) Safety and side effects of cannabidiol, a
Cannabis sativa constituent. Curr Drug Saf 6:237–249
Borea PA, Varani K, Vincenzi F, Baraldi PG, Tabrizi MA, Merighi S, Gessi S (2015) The A3 adenosine receptor:
history and perspectives. Pharmacol Rev 67:74–102
Boyd KN, Mailman RB (2012) Dopamine receptor signaling and current and future antipsychotic drugs.
Handb Exp Pharmacol 212:53–86
Brown SP, Safo PK, Regehr WG (2004) Endocannabinoids inhibit transmission at granule cell to Purkinje
cell synapses by modulating three types of presynaptic calcium channels. J Neurosci 24:5623–5631
Catterall WA (2015) Regulation of cardiac calcium channels in the fight-or-flight response. Curr Mol
Pharmacol 8:12–21
extracellular ligand for adenosine receptors, it signals in an energy-dependent
way to induce physiological and psychological responses, such as modulation of
motor activity and sleep.
5 Cannabis (THC) from the plant Cannabis sativa partially agonizes cannabinoid
receptors. Cannabinoid receptors are activated by endogenous cannabinoids
including arachidonoylglycerol and anandamide, both derivatives of arachidonic
acid. They are released from the postsynapse after neurotransmission at both,
activating (glutamate) or inhibiting (GABA) synapses. Cannabinoid receptors at
the presynapse are activated in response and block secretion of the neurotransmitter. This system comprises a paradigm for retrograde neuronal signalling.
5 Cocaine and the synthetic drugs amphetamine and methamphetamine inhibit
the dopamine transporter DAT. DAT is a solute carrier transporter and a Na + /
dopamine symporter. It regulates the availability of dopamine, serotonin and
noradrenalin for synaptic signalling on receptors by transporting it from the
synaptic cleft back into the cell. Its inhibition therefore induces a dopamine
“overflow” and this may cause euphoria and increased activity and performance.
Side effects relate to disturbed uptake of noradrenalin and include increases in
breathing and heart frequency.
5 Hallucinogens include psilocybin, mescaline and the synthetic drug LSD. They
act preferably on 5HT2 A receptors which are GPCRs. Their activation leads to a
robust increase in the activity of pyramidal neurons, which receive input from
brain areas processing sensory information. This induces a sensory and cognitive
overload.
5 Morphine and other opioids bind to opioid receptors. Opioid receptors are activated
by endogenous peptides including enkephalins. They are involved in modulating
pain perception. Morphine is the agonist for the μ-opioid receptors. It has strong
analgesic effects. Acting on opioid receptors in certain brain regions, it also causes
euphoria and feelings of pleasure and reward. On the downside it induces tolerance, addiction and extremely strong withdrawal symptoms after extended usage.
Chapter 5 · GPCRs as Targets for Plant-Derived Drugs