Cholinergic receptor subtypes in the urinary bladder of the rat in situ

J. López, A. Correa, G. Pinardi, H. F. Miranda

Resultado de la investigación: Article

Resumen

The published evidence on the contractile response of the isolated urinary bladder in vitro suggests that neurotransmission in the smooth muscle is complex. The present work attempts to characterize muscarinic receptor subtypes involved in the contractile response of the whole urinary bladder of the rat in situ, using selective muscarinic antagonists. The intra-arterial administration of acetylcholine (ACh, 0.001 - 3 mg/kg) or carbachol (CCh, 0.001 - 1 mg/kg) produced a dose-dependent contraction with EC50 values (ACh: 0.028 mg/kg, CCh: 0.024 mg/kg) and Emax values not significantly different (2.02 ± 0.16 g for ACh, n = 46 and 1.86 ± 0.14 g for CCh, n = 48; P > 0.05). The pretreatment of the rat with the M1 selective antagonist PZP (0.238, 0.714, 2.38 or 714 μM) produced an antagonism characterized by apparent pA2 values of 6.77 ± 0.14 (n = 24) and 4.86 ± 0.28 (n = 28), for ACh and CCh, respectively. When the rat was pretreated with the M3 selective antagonist, p-FHHSD (0.238, 0.783 and 2.61 μM), apparent pA2 values of 6.07 ± 0.11 for ACh (n = 18) and 6.19 ± 0.48 (n = 20) for CCh were found. With the M2 selective antagonist AFDX-116 (0.239, 0717 and 2.39 μM), the corresponding apparent pA2values were 5.30 ± 0.19 (n = 24), in the case of ACh and 5.02 ± 0.31 (n = 22), in the case of CCh. The results obtained demostrate that ACh-induced contractile responses in the rat urinary bladder in situ are due mainly to the activation of ACh-M1and ACh-M3 receptor subtypes, while CCh contractile responses seem to be due to the activation of ACh-M3 and/or ACh-M2 receptor subtypes.

Idioma originalEnglish
Páginas (desde-hasta)65-70
Número de páginas6
PublicaciónPharmacology Reviews and Communications
Volumen11
N.º1
EstadoPublished - 2000

Huella dactilar

Cholinergic Receptors
Urinary Bladder
Muscarinic Antagonists
Carbachol
Muscarinic Receptors
Synaptic Transmission
Acetylcholine
Smooth Muscle

ASJC Scopus subject areas

  • Pharmacology

Citar esto

López, J., Correa, A., Pinardi, G., & Miranda, H. F. (2000). Cholinergic receptor subtypes in the urinary bladder of the rat in situ. Pharmacology Reviews and Communications, 11(1), 65-70.
López, J. ; Correa, A. ; Pinardi, G. ; Miranda, H. F. / Cholinergic receptor subtypes in the urinary bladder of the rat in situ. En: Pharmacology Reviews and Communications. 2000 ; Vol. 11, N.º 1. pp. 65-70.
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López, J, Correa, A, Pinardi, G & Miranda, HF 2000, 'Cholinergic receptor subtypes in the urinary bladder of the rat in situ', Pharmacology Reviews and Communications, vol. 11, n.º 1, pp. 65-70.

Cholinergic receptor subtypes in the urinary bladder of the rat in situ. / López, J.; Correa, A.; Pinardi, G.; Miranda, H. F.

En: Pharmacology Reviews and Communications, Vol. 11, N.º 1, 2000, p. 65-70.

Resultado de la investigación: Article

TY - JOUR

T1 - Cholinergic receptor subtypes in the urinary bladder of the rat in situ

AU - López, J.

AU - Correa, A.

AU - Pinardi, G.

AU - Miranda, H. F.

PY - 2000

Y1 - 2000

N2 - The published evidence on the contractile response of the isolated urinary bladder in vitro suggests that neurotransmission in the smooth muscle is complex. The present work attempts to characterize muscarinic receptor subtypes involved in the contractile response of the whole urinary bladder of the rat in situ, using selective muscarinic antagonists. The intra-arterial administration of acetylcholine (ACh, 0.001 - 3 mg/kg) or carbachol (CCh, 0.001 - 1 mg/kg) produced a dose-dependent contraction with EC50 values (ACh: 0.028 mg/kg, CCh: 0.024 mg/kg) and Emax values not significantly different (2.02 ± 0.16 g for ACh, n = 46 and 1.86 ± 0.14 g for CCh, n = 48; P > 0.05). The pretreatment of the rat with the M1 selective antagonist PZP (0.238, 0.714, 2.38 or 714 μM) produced an antagonism characterized by apparent pA2 values of 6.77 ± 0.14 (n = 24) and 4.86 ± 0.28 (n = 28), for ACh and CCh, respectively. When the rat was pretreated with the M3 selective antagonist, p-FHHSD (0.238, 0.783 and 2.61 μM), apparent pA2 values of 6.07 ± 0.11 for ACh (n = 18) and 6.19 ± 0.48 (n = 20) for CCh were found. With the M2 selective antagonist AFDX-116 (0.239, 0717 and 2.39 μM), the corresponding apparent pA2values were 5.30 ± 0.19 (n = 24), in the case of ACh and 5.02 ± 0.31 (n = 22), in the case of CCh. The results obtained demostrate that ACh-induced contractile responses in the rat urinary bladder in situ are due mainly to the activation of ACh-M1and ACh-M3 receptor subtypes, while CCh contractile responses seem to be due to the activation of ACh-M3 and/or ACh-M2 receptor subtypes.

AB - The published evidence on the contractile response of the isolated urinary bladder in vitro suggests that neurotransmission in the smooth muscle is complex. The present work attempts to characterize muscarinic receptor subtypes involved in the contractile response of the whole urinary bladder of the rat in situ, using selective muscarinic antagonists. The intra-arterial administration of acetylcholine (ACh, 0.001 - 3 mg/kg) or carbachol (CCh, 0.001 - 1 mg/kg) produced a dose-dependent contraction with EC50 values (ACh: 0.028 mg/kg, CCh: 0.024 mg/kg) and Emax values not significantly different (2.02 ± 0.16 g for ACh, n = 46 and 1.86 ± 0.14 g for CCh, n = 48; P > 0.05). The pretreatment of the rat with the M1 selective antagonist PZP (0.238, 0.714, 2.38 or 714 μM) produced an antagonism characterized by apparent pA2 values of 6.77 ± 0.14 (n = 24) and 4.86 ± 0.28 (n = 28), for ACh and CCh, respectively. When the rat was pretreated with the M3 selective antagonist, p-FHHSD (0.238, 0.783 and 2.61 μM), apparent pA2 values of 6.07 ± 0.11 for ACh (n = 18) and 6.19 ± 0.48 (n = 20) for CCh were found. With the M2 selective antagonist AFDX-116 (0.239, 0717 and 2.39 μM), the corresponding apparent pA2values were 5.30 ± 0.19 (n = 24), in the case of ACh and 5.02 ± 0.31 (n = 22), in the case of CCh. The results obtained demostrate that ACh-induced contractile responses in the rat urinary bladder in situ are due mainly to the activation of ACh-M1and ACh-M3 receptor subtypes, while CCh contractile responses seem to be due to the activation of ACh-M3 and/or ACh-M2 receptor subtypes.

KW - Acetylcholine

KW - AFDX-116

KW - Carbachol

KW - P-FHHSiD

KW - Pirenzepine

KW - Urinary bladder

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