TABLE 7

Comparison of binding pockets of neurokinin, bradykinin, and vasopressin

The key amino acids located at helix positions in the Ballesteros numbering (Ballesteros and Weinstein, 1995) that have been implicated in the peptide agonist and selective nonpeptide antagonist binding pockets were compared among hNK₁R, hNK₂R, hNK₃R, bradykinin B2 receptor, hV_1aR, and hV_1bR. The hNK₃R data are from current study

Position in the 7TMD	hNK₁R	hNK₂R					hNK₃R					Human Bradykinin B2 Receptor	hV_1aR
Position in the 7TMD		SP^a	NKA^b	Saredutant^c	MEM13510^d	NKB	Me-Talnetant	Osanetant	FR173657^e	AVP^f	SR49059^g	AVP^f	SR149415^h
2.57	Asn85	Asn86			Asn138
2.61	Asn89	Asn90			Asn142		Asn142		Gln108		Gln91
3.36						Val169	Val169		Met135	Met135	Met118	Met118
6.51		Tyr266	Tyr266		Tyr315	Tyr315	Tyr315		Phe307	Phe307	Phe297	Phe297
7.39		Phe293		Phe293	Phe342	Phe342	Phe342			Ala334ⁱ		Met324
7.43		Met297			Met346			Tyr295				Asn328

Reported data are from:
↵ a Huang et al. (1994).
↵ b Huang et al. (1995); Labrou et al. (2001).
↵ c Renzetti et al. (1999).
↵ d Meini et al. (2005).
↵ e Meini et al. (2004).
↵ f Mouillac et al. (1995).
↵ g Tahtaoui et al. (2003).
↵ h Derick et al. (2004).
↵ i Ala334 is the crucial residue for selectivity SR49059 for hV_1aR over hV_1bR (Derick et al., 2004).