Distribution and pharmacological characterization of muscarinic-cholinergic receptors in the cockroach brain
The binding of [3H]quinuclidinyl benzilate to a cockroach brain preparation was investigated. Specific binding was saturable with a Kd of 0.25 nM and Scatchard analysis indicated a Bmax of 604 pmol/mg protein. Kinetic analysis indicated that the ligand is binding in a complex fashion while dissociat...
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Published in | Archives of insect biochemistry and physiology Vol. 16; no. 2; p. 107 |
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Main Authors | , , |
Format | Journal Article |
Language | English |
Published |
United States
1991
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Abstract | The binding of [3H]quinuclidinyl benzilate to a cockroach brain preparation was investigated. Specific binding was saturable with a Kd of 0.25 nM and Scatchard analysis indicated a Bmax of 604 pmol/mg protein. Kinetic analysis indicated that the ligand is binding in a complex fashion while dissociation followed a simple kinetic process. The pharmacology of the site was typical of muscarinic receptors but the site cannot be characterized in terms of vertebrate muscarinic-receptor subtypes. Affinity of the receptor for agonists was modulated by Mg2+ and guanylylimidodiphosphate but not by pertussis toxin indicating the involvement of a pertussis-toxin insensitive G-protein. Carbamylcholine did not inhibit basal or forskolin-stimulated adenylate cyclase activity. The binding site was localized autoradiographically and was restricted to the median and lateral calyces of the brain |
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AbstractList | The binding of [3H]quinuclidinyl benzilate to a cockroach brain preparation was investigated. Specific binding was saturable with a Kd of 0.25 nM and Scatchard analysis indicated a Bmax of 604 pmol/mg protein. Kinetic analysis indicated that the ligand is binding in a complex fashion while dissociation followed a simple kinetic process. The pharmacology of the site was typical of muscarinic receptors but the site cannot be characterized in terms of vertebrate muscarinic-receptor subtypes. Affinity of the receptor for agonists was modulated by Mg2+ and guanylylimidodiphosphate but not by pertussis toxin indicating the involvement of a pertussis-toxin insensitive G-protein. Carbamylcholine did not inhibit basal or forskolin-stimulated adenylate cyclase activity. The binding site was localized autoradiographically and was restricted to the median and lateral calyces of the brain The binding of [3H]quinuclidinyl benzilate to a cockroach brain preparation was investigated. Specific binding was saturable with a Kd of 0.25 nM and Scatchard analysis indicated a Bmax of 604 pmol/mg protein. Kinetic analysis indicated that the ligand is binding in a complex fashion while dissociation followed a simple kinetic process. The pharmacology of the site was typical of muscarinic receptors but the site cannot be characterized in terms of vertebrate muscarinic-receptor subtypes. Affinity of the receptor for agonists was modulated by Mg2+ and guanylylimidodiphosphate but not by pertussis toxin indicating the involvement of a pertussis-toxin insensitive G-protein. Carbamylcholine did not inhibit basal or forskolin-stimulated adenylate cyclase activity. The binding site was localized autoradiographically and was restricted to the median and lateral calyces of the brain. |
Author | Hollingworth, R.M Orr, G.L. (Michigan State University, East Lansing, MI) Orr, N |
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CitedBy_id | crossref_primary_10_1515_bchm3_1996_377_12_819 crossref_primary_10_1007_s00359_008_0411_6 crossref_primary_10_1242_jeb_181_1_257 crossref_primary_10_1002__SICI_1096_9063_199703_49_3_268__AID_PS527_3_0_CO_2_C crossref_primary_10_1016_0166_2236_95_80032_W crossref_primary_10_1016_j_neubiorev_2012_04_003 crossref_primary_10_1007_BF00188693 crossref_primary_10_1016_S0965_1748_96_00042_2 crossref_primary_10_1152_jn_00963_2009 crossref_primary_10_3390_insects13090806 crossref_primary_10_1016_j_pestbp_2009_04_009 crossref_primary_10_1016_0742_8413_95_00070_4 crossref_primary_10_1111_j_1365_2826_1995_tb00768_x crossref_primary_10_1007_BF02336662 crossref_primary_10_1002_neu_480280406 crossref_primary_10_1016_0304_3940_94_91104_5 crossref_primary_10_1016_j_cca_2004_03_002 |
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Snippet | The binding of [3H]quinuclidinyl benzilate to a cockroach brain preparation was investigated. Specific binding was saturable with a Kd of 0.25 nM and Scatchard... |
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SubjectTerms | ACETILCOLINA ACETYLCHOLINE Animals Autoradiography Binding, Competitive Brain - metabolism Bungarotoxins - metabolism CEREBRO Cockroaches - metabolism Cyclic AMP - metabolism ENCEPHALE Kinetics LIGAND LIGANDOS MACHO MALE MEDICAMENT NEUROTROPE MEDICAMENTOS NEUROTROPICOS PERIPLANETA AMERICANA Quinuclidinyl Benzilate - metabolism RADIOGRAFIA RADIOGRAPHIE Receptors, Muscarinic - metabolism Receptors, Nicotinic - metabolism TECHNIQUE DES TRACEURS TECNICAS DE TRAZADORES Tritium |
Title | Distribution and pharmacological characterization of muscarinic-cholinergic receptors in the cockroach brain |
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