TABLE 3

Potencies of H₃R agonists and antagonists

For recombinant receptors all values refer to the full-length (445 aa) receptor.

Drug	pIC₅₀ or pEC₅₀					pA₂	pK_B	pD₂
Drug	cAMP	Ca²⁺	MAPK	GTPγS	PI3K/ Akt	pA₂	pK_B	pD₂
RAMH	8.50 ± 0.10 (r)^{^a}	8.44 ± 0.11^b	7.94 ± 0.17 (h)^{^c}	8.50 ± 0.14 (h)^{^c}				7.60 ± 0.05^{^d}
	9.50 ± 0.10^{^e}	7.92^{^f}		8.00 ± 0.10^{^g}				8.50 ± 0.10^{^a}
	9.17 ± 0.03^{^h}	8.22^{^f}		7.65 (r)^{^f}
	8.22 ± 0.35 (h)^{^c}	8.50 ± 0.13^ⁱ		8.02, 8.42 (h)^{^f}
	8.20 ± 0.10^{^g}
	8.67 (r)^{^f}
	8.01 (h)^{^f}
	9.47 ± 0.18^ⁱ
	9.54 ± 0.06^{^j}
SAMH	8.00 ± 0.10^{^e}			6.60 ± 0.10^{^g}				6.21 ± 0.15^{^d}
	6.80 ± 0.10^{^g}
	8.31 ± 0.01^{^j}
Histamine	8.30 ± 0.10^{^e}	7.66, 7.81, 7.75, 7.76^{^k}		7.30 ± 0.10^{^g}				6.46 ± 0.18^{^d}
	8.01 ± 0.03^{^h}	7.99 ± 0.09^{^b}						7.40 ± 0.10^{^l}
	7.40 ± 0.20^{^g}	7.82 ± 0.09^ⁱ
	8.63 ± 0.10^ⁱ
	8.55 ± 0.05^{^j}
Imetit	9.90 ± 0.10^{^e}	8.13, 8.03, 8.40, 8.48^{^k}		8.60 ± 0.10^{^g}				7.80 ± 0.10^{^d}
	9.66 (r)^{^f}	8.47 ± 0.08^b		8.69 (r)^{^f}
	8.39 (h)^{^f}	8.14^{^f}		8.53, 8.71 (h)^{^f}
	8.92 ± 0.04^{^m}	8.04^{^f}
	9.79 ± 0.20^ⁱ	8.86 ± 0.20^ⁱ
	9.91 ± 0.05^{^j}
Immepip	9.40 ± 0.10 (r)^{^a}			8.80 ± 0.10^{^g}	9.40^ⁿ			8.35 ± 0.08^{^d}
	10.40 ± 0.10^{^e}							9.40 ± 0.10^{^a}
	9.88 ± 0.02^{^h}
	9.00 ± 0.10^{^g}
	9.90 ± 0.10^ⁿ
	9.90 ± 0.0^{^o}
	7.88^{^q}
	10.30 ± 0.14^{^j}
Impentamine	8.1 (r)^{^a}			7.50 ± 0.10^{^q}
	8.40 ± 0.10^{^e}							8.10 ± 0.10^{^a}
	8.63 ± 0.08^{^h}
	9.17 ± 0.11^ⁱ
	8.43 ± 0.08^{^j}
NAMH	9.40 ± 0.10^{^e}	8.03, 8.15, 8.34, 8.22^{^k}		7.90 ± 0.10^{^g}				7.17 ± 0.07^{^d}
	8.50 ± 0.10^{^g}
	9.45 ± 0.05^{^j}
Methimepip	9.50 ± 0.20^{^e}
Methimepip	9.50 ± 0.20^{^o}
VUF 5296	7.24 ± 0.04^{^h}							6.15 ± 0.08^{^l}
VUF 5297	8.23 ± 0.14^{^h}							6.64 ± 0.06^{^l}
Proxyfan	8.50 ± 0.10^{^e}	7.43 ± 0.06^{^b}		7.50 ± 0.10^{^g}
	7.83(r)^{^f}	7.61, 7.11^{^f}		7.33 (r)^{^f}
	6.86 (h)^{^f}	6.20, 5.89^{^f}		7.49, 7.68 (h)^{^f}
	7.73^{^f}
	7.61^{^f}
	8.31 ± 0.11^{^j}
Thioperamide	7.50 ± 0.10^{^e}			8.06 ± 0.10 (r)^{^q}	7.00^ⁿ	8.44 ± 0.45^{^d}	6.90 ± 0.10^{^t}
	7.60 ± 0.20^{^g}			7.41 ± 0.11 (h)^{^q}		8.44 ± 0.49 (gp)^{^r}	8.13 ± 0.14 (r)^{^q}
	7.10 ± 0.20^ⁿ			6.90 ± 0.10^{^g}			7.39 ± 0.04 (h)^{^q}
	7.88^{^p}			7.49 ± 0.34^{^s}			9.11 ± 0.14 (r)^{^q}
				7.41 ± 0.12 (h)^{^t}			6.82 ± 0.05 (h)^{^q}
				8.06 ± 0.10 (r)^{^t}			7.09 ± 0.08 (mk)^{^b}
							6.82 ± 0.06 (h)^{^t}
							6.10 ± 0.12 (h)^{^t}
							7.39 ± 0.04 (h)^{^t}
							6.82 ± 0.06 (h)^{^t}
							7.61 ± 0.14 (r)^{^t}
							8.13 ± 0.14 (r)^{^t}
							8.95^{^v}
Ciproxifan	5.39, 5.30^{^f}	6.57, 6.58^{^f}		8.87 ± 0.16 (r)^{^q}		8.12 ± 0.56^{^d}	8.78 ± 0.12 (r)^{^q}
				7.04 ± 0.17 (h)^{^q}		8.12 ± 0.56^{^s}	7.03 ± 0.13 (h)^{^q}
				7.16 ± 0.19^{^s}			9.42 ± 0.11 (r)^{^q}
				7.04 ± 0.17 (h)^{^s}			6.86 ± 0.07 (h)^{^q}
				8.87 ± 0.16 (r)^{^s}			7.23 ± 0.04 (mk)^{^b}
							9.10 (r)^{^f}
							6.59 (h)^{^f}
							6.84 ± 0.08^{^t}
							6.59 ± 0.04 (h)^{^s}
							7.07 ± 0.13 (h)^{^s}
							6.84 ± 0.08 (h)^{^s}
							9.20 ± 0.10 (r)^{^s}
							8.78 ± 0.12 (r)^{^s}
Burimamide	7.00 ± 0.10^{^e}					8.05 ± 0.68^{^d}	7.56^{^v}
Burimamide	6.65 ± 0.10^{^j}					8.05 ± 0.68^{^d}	7.56^{^v}
Iodophenpropit	8.50 ± 0.10^{^e}					9.14 ± 0.61^{^d}
Iodophenpropit	8.50 ± 0.40^{^g}					9.14 ± 0.61^{^d}
Iodoproxyfan	10.30 ± 0.10^{^e}
Clobenpropit	9.40 ± 0.10^{^e}	7.41, 7.10^{^f}		8.07 ± 0.66^{^t}		9.66 ± 0.49^{^d}	9.80 ± 0.03 (mk)^{^b}
	6.79, 6.55^{^f}					9.66 ± 0.49^{^t}	9.03 (r)^{^f}
							8.35 (h)^{^f}
							8.21 ± 0.10 (h)^{^t}
							9.04 ± 0.11 (r)^{^t}
							8.91 ± 0.06 (h)^{^t}
VUF 5681	8.41 ± 0.10^{^j}					8.08 ± 0.03^{^h}
A-331440				7.07 ± 0.24 (r)^{^q}	7.70^ⁿ		7.60 ± 0.12 (r)^{^q}
				7.70 ± 0.08 (h)^{^q}			8.16 ± 0.04 (h)^{^q}
							7.38 ± 0.10 (r)^{^q}
				7.60 ± 0.10^{^g}			7.37 ± 0.29 (h)^{^q}
							7.81 ± 0.02 (mk)^{^b}
A-349821	9.00 ± 0.40^{^g}			9.20 ± 0.10^{^g}		9.47 ± 0.56^{^s}	9.67 ± 0.05 (mk)^{^b}
				9.09 ± 0.08 (h)^{^s}			8.27 ± 0.12^{^u}
				8.57 ± 0.09 (r)^{^s}			8.24 ± 0.10 (h)^{^s}
							9.26 ± 0.02 (h)^{^s}
							8.27 ± 0.12^{^r} (h)^{^s}
							8.08 ± 0.10 (r)^{^s}
							8.62 ± 0.11 (r)^{^s}
ABT-229							7.87 ± 0.15 (r)^{^u}
							7.89 ± 0.04 (h)^{^w}
							9.04 ± 0.04 (h)^{^w}
							7.87 ± 0.15 (h)^{^w}
							7.60 ± 0.05 (r)^{^w}
							8.34 ± 0.14 (r)^{^w}
							8.74 ± 0.44 (gp)^{^w}
GSK189254				8.20 ± 0.12^{^m}		9.06 ± 0.02^{^m}
JNJ-5207852						8.94 (r)^{^x}
JNJ-5207852						9.84 (h)^{^x}
NCC 38-1049							8.63^{^y}
Pitolisant							9.79^{^z}

Gp, guinea pig; h, human; mk, monkey; NAMH, N^α-methylhistamine; r, rat.
↵^a Drutel et al., 2001.
↵^b Strakhova et al., 2008.
↵^c Flores-Clemente et al., 2013.
↵^d Ireland-Denny et al., 2001.
↵^e Lim et al., 2005.
↵^f Krueger et al., 2005.
↵^g Bongers et al., 2007b.
↵^h Kitbunnadaj et al., 2003.
↵ⁱ Uveges et al., 2002.
↵^j Baker, 2008.
↵^k Chen et al., 2003.
↵^l De Esch et al., 1999.
↵^m Medhurst et al., 2007.
↵ⁿ Bongers et al., 2007c.
↵^o Kitbunnadaj et al., 2005.
↵^p Sánchez-Lemus and Arias-Montaño, 2004.
↵^q Hancock et al., 2004a.
↵^r Lovenberg et al., 2000.
↵^s Esbenshade et al., 2004.
↵^t Esbenshade et al., 2003.
↵^u Cowart et al., 2005.
↵^v Hew et al., 1990.
↵^w Esbenshade et al., 2005.
↵^x Barbier et al., 2004.
↵^y Malmlöf et al., 2005.
↵^z Ligneau et al., 2007.