author={Issei Takayanagi and Katsuo Koike and Mitsutoshi Satoh},
  journal={Journal of Smooth Muscle Research},
It is generally accepted that the agonists, full agonist and partial agonist, interact with the same receptors according to the classical receptor mechanisms. We tried to modify the drug receptor mechanisms in muscarinic cholinoceptors, α1-adrenoceptors and β-adrenoceptors. In the muscarinic cholinoceptor, there are two subtypes of M3-cholinoceptors, propylbenzilylcholine mustard (PrBCM)-sensitive receptors and PrBCM-resistant ones. The full agonists contract the longitudinal muscle through the… 
1 Citation

Propylbenzilycholine mustard (PrBCM)-sensitive cholinoceptors and contractile response to partial agonist in guinea pig ileal muscle.

The slopes of the regression lines between [Ca2+]i and tension development for pilocarpine in the untreated preparation and for carbachol in the preparation treated with phenoxybenzamine were significantly steeper than that for carb cholinoceptors in the treated preparation, suggesting that carbachols in the phenoxy Benzamine-treated preparation induced a greater tension for a given increase in low Ca2+i than did carbACHol.

A possible mechanism of action of a beta-adrenergic partial agonist (carteolol) in guinea pig taenia caecum.

Carteolol, 5-(3-tert-butylamino-2-hydroxy)propoxy-3, 4-dihydrocarbostyril hydrochloride was found to be a beta-adrenergic partial agonist in the taenia caecum of guinea pig. Concentration response

Interactions of some partial agonists with high and low affinity binding sites in beta-adrenoceptors.

BFE-61, carteolol, and pindolol discriminate between the two affinity binding sites in the beta-adrenoceptors, which are not discriminated between by BFE-37, and further that B FE-55 may bind with only the high affinity site.

A possible mechanism in interaction of a partial agonist with beta-adrenoceptor in guinea-pig taenia caecum: effects of Gpp(NH)p on its two different binding sites.

The results suggest that the beta-adrenergic partial agonist may interact with two different sites: an agonist binding site and an antagonist binding site.

Interactions of some partial agonists with beta-adrenoceptor in the isolated taenia caecum and tracheal smooth muscle of guinea pig.

The results suggest that the properties of the binding site for agonistic action were different from those for antagonistic action, and that the partial agonists had little receptor reserve.

Pharmacological subclassification of α1‐adrenoceptors in vascular smooth muscle

The results suggest that α1 ‐adrenoceptors of blood vessels can be divided into three subtypes (designated as α1H, α1L and α1N) by antagonist affinity and their susceptibility to chloroethylclonidine but not to nifedipine.

Selectivity of muscarinic antagonists in radioligand and in vivo experiments for the putative M1, M2 and M3 receptors.

It is proposed that there are three different binding sites present in hippocampal, atrial and submandibular membranes and it is suggested to classify them as M1, M2 and M3, respectively.