The Concise Guide to Pharmacology 2013/14: G Protein-Coupled Receptors

. 2013 Dec 17;170(8):1459–1581. doi: 10.1111/bph.12445

Nomenclature	5-HT1A receptor	5-HT1B receptor	5-HT1D receptor	5-ht1e receptor	5-HT1F receptor
HGNC, UniProt	HTR1A, P08908	HTR1B, P28222	HTR1D, P28221	HTR1E, P28566	HTR1F, P30939
Principal transduction	G_i/o	G_i/o	G_i/o	G_i/o	G_i/o
Selective agonists (pK_i)	U92016A (9.7) 178, 8-OH-DPAT (8.4 – 9.4) 140,151,170,183,189,191,192, F15599 (8.6) 190	L-694,247 (9.2) 149, CP94253 (8.7) 167, eletriptan (8.0) 184, sumatriptan (Partial agonist) (6.5 – 8.1) 149,172,183,184,187,194,215	PNU109291 (9.1 - Gorilla) 143, L-694,247 (9.0) 217, eletriptan (8.9) 184, sumatriptan (8.0 – 8.7) 150,172,183,184,215	BRL-54443 (8.7) 136	BRL-54443 (8.9) 136, LY334370 (8.7) 213, LY573144 (8.7) 186, LY344864 (8.2) 195, eletriptan (8.0) 184, sumatriptan (7.2 – 7.9) 114,115,184,213
Selective antagonists (pK_i)	NAD 299 (9.2) 161, WAY-100635 (7.9 – 9.2) 189,191, (S)-UH 301 (7.9) 189	GR-55562 (pK_B 7.4) 159, SB 224289 (Inverse agonist) (8.2 – 8.6) 146,187,203, SB236057 (Inverse agonist) (8.2) 182	SB 714786 (9.1) 214, BRL-15572 (7.9) 196	–	–
Radioligands (K_d)	p-[18F]MPPF, [11C]WAY100635 (Antagonist), [3H]NAD 299 (Antagonist) (1.58x10^-10 M) 160, [3H]WAY100635 (Antagonist) (3x10^-10 M) 164, [3H]F13640 (Agonist, Full agonist) (1.4x10^-9 M) 155, [3H]8-OH-DPAT (Agonist, Full agonist) (3.98x10^-10 – 1x10^-6 M) 122,162,188,191	[11C]AZ10419369, [3H]N-methyl-AZ10419369 (Antagonist) (3.7x10^-10 M) 175, [125I]GTI (Agonist) (1.3x10^-9 M - Rat) 130, [3H]GR 125,743 (Antagonist) (2.6x10^-9 – 7.1x10^-10 M) 149,218, [3H]alniditan (Agonist, Full agonist) (1x10^-9 – 2.51x10^-9 M) 171, [3H]eletriptan (Agonist, Partial agonist) (3x10^-9 M) 184, [3H]sumatriptan (Agonist, Partial agonist) (1.1x10^-8 M) 184	[3H]eletriptan (Agonist, Full agonist) (9x10^-10 M) 184, [125I]GTI (Agonist) (1.3x10^-9 M - Rat) 130, [3H]alniditan (Agonist, Full agonist) (1.2x10^-9 – 1.4x10^-9 M) 171, [3H]GR 125,743 (Antagonist) (2.8x10^-9 M) 218, [3H]sumatriptan (Agonist, Full agonist) (7x10^-9 M) 184	[3H]5-HT (Agonist, Full agonist) (6.31x10^-9 – 7.94x10^-9 M) 177,194	[3H]LY334370 (Agonist, Full agonist) (3.98x10^-10 M) 213, [125I]LSD (Agonist) (9.8x10^-10 M - Mouse) 116