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. Author manuscript; available in PMC: 2021 May 4.
Published in final edited form as: Curr Opin Pharmacol. 2020 May 4;51:19–28. doi: 10.1016/j.coph.2020.04.002

Table 1:

Class C GPCR Members

Member Pharmacological Modulators Dimerization Roles in Lung
Metabotropic GABA:
GABABR1, GABABR2
Ligand: GABA
Agonist: Baclofen, CGP27492
Antagonist: Phaclofen, Saclofen, CGP36742, CGP35348, CGP55845
PAM: CGP7930
Heterodimer ASM and epithelium
↑ airway contractility
↑ mucus production
CaSR Ligand: Ca2+, spermine
Agonist: Ca2+, Mg2+, polyvalent cations, β-amyloid, aminoglycoside antibiotics
PAM: pH, L-α-amino acids, NPS R467, NPS R568, cinacalcet
NAM: NPS 2143, Calhex 231
Homodimer Heterodimer (mGlu Grp I) ASM and epithelium
↑ airway and pulmonary vascular contractility
↑ cell proliferation
↑ airway fluid secretion
↑ epithelial inflammation
GPRC6A Ligand: L-α-amino acid Homodimer Unkno ‘n
Sweet/Umami Taste:
T1R1, T1R2, T1R3
Ligand: T1R1/T1R3: L-glutamate; T1R2/T1R3: Sugars Homodimer Heterodir er (T1R1/T1R3, T1R2/T1R3) Unknown
(potential airway immune modulation)
Metabotropic Glutamate Grp I:
mGluR1, mGluR5
Ligand: Glutamate, ACPD
Agonist: DHPG, CHPG, LY339764
Antagonist: CPPCOEt, BAY36–7620, Ro 674853
Homodimer PHetei’dimer (‘rp |’, III) Unknown
Metabotropic Glutamate Grp II:
mGluR2, mGluR3
Ligand: Glutamate, ACPD
Agonist: LY341495, LY354740
Antagonist: Ro 64–5229, LY487379
Homodimer Unknown
Metabotropic Glutamate Grp III
mGluR4, mGluR6, mGluR7, mGluR8
Ligand: Glutamate, ACPD
Agonist: MAP4, DCPG
Antagonist: PHCCC
Homodimer Unknown
RAIG Orphan: GPRC5A, GPRC5B, GPRC5C, GPRC5D Unknown Unknown Unknown (GPRC5A may be most relevant)
Other Orphan: GPR156, GPR158, GPR179 Unkno n Unknown Unknown